Identification

Name
Mianserin
Accession Number
DB06148
Type
Small Molecule
Groups
Approved, Investigational
Description

A tetracyclic compound with antidepressant effects. Mianserin was previously available internationally, however in most markets it has been phased out in favor of Mirtazapine.

Structure
Thumb
Synonyms
  • 1,2,3,4,10,14b-Hexahydro-2-methyldibenzo(c,F)pyrazino(1,2-a)azepine
  • Mianserina
  • Mianserine
  • Mianserinum
  • Mianseryna
Product Ingredients
IngredientUNIICASInChI Key
Mianserin hydrochloride2X03TN217S21535-47-7YNPFMWCWRVTGKJ-UHFFFAOYSA-N
International/Other Brands
Bolvidon / Depnon / Lantanon / Lumin / Norval / Tolvon
Categories
UNII
250PJI13LM
CAS number
24219-97-4
Weight
Average: 264.3648
Monoisotopic: 264.16264865
Chemical Formula
C18H20N2
InChI Key
UEQUQVLFIPOEMF-UHFFFAOYSA-N
InChI
InChI=1S/C18H20N2/c1-19-10-11-20-17-9-5-3-7-15(17)12-14-6-2-4-8-16(14)18(20)13-19/h2-9,18H,10-13H2,1H3
IUPAC Name
5-methyl-2,5-diazatetracyclo[13.4.0.0²,⁷.0⁸,¹³]nonadeca-1(19),8,10,12,15,17-hexaene
SMILES
CN1CCN2C(C1)C1=CC=CC=C1CC1=CC=CC=C21

Pharmacology

Indication

For the treatment of depression.

Structured Indications
Not Available
Pharmacodynamics

Mianserin is a tetracyclic antidepressant that has antihistaminic and hypnosedative, but almost no anticholinergic, effect. It is a weak inhibitor of norepinephrine reuptake and strongly stimulates the release of norepinephrine. Interactions with serotonin receptors in the central nervous system have also been found. Its effect is usually noticeable after one to three weeks. Mianserin may cause drowsiness and hematological problems.

Mechanism of action

Mianserin's mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.

TargetActionsOrganism
UAlpha-2A adrenergic receptor
antagonist
Human
U5-hydroxytryptamine receptor 2A
antagonist
Human
U5-hydroxytryptamine receptor 2C
antagonist
Human
UHistamine H1 receptor
antagonist
Human
USodium-dependent noradrenaline transporter
inhibitor
Human
USodium-dependent serotonin transporter
inhibitor
Human
UHistamine H4 receptor
binder
Human
U5-hydroxytryptamine receptor 1A
blocker
Human
UAlpha-2C adrenergic receptor
antagonist
Human
U5-hydroxytryptamine receptor 2B
binder
Human
U5-hydroxytryptamine receptor 1F
binder
Human
UAlpha-2B adrenergic receptor
antagonist
Human
UD(3) dopamine receptor
binder
Human
UKappa-type opioid receptor
agonist
Human
USodium-dependent dopamine transporter
binder
Human
U5-hydroxytryptamine receptor 7
antagonist
Human
UD(2) dopamine receptor
antagonist
Human
U5-hydroxytryptamine receptor 6
binder
Human
UAlpha-1 adrenergic receptors
antagonist
Human
UD(1) dopamine receptor
binder
Human
Absorption

Absorbed following oral administration.

Volume of distribution
Not Available
Protein binding

90%

Metabolism

Hepatic.

Route of elimination
Not Available
Half life

10-17 hours

Clearance
Not Available
Toxicity

Oral rat LD50: 780mg/kg

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamine2,5-Dimethoxy-4-ethylamphetamine may decrease the sedative activities of Mianserin.Experimental, Illicit
3,4-Methylenedioxyamphetamine3,4-Methylenedioxyamphetamine may decrease the sedative activities of Mianserin.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamine4-Bromo-2,5-dimethoxyamphetamine may decrease the sedative activities of Mianserin.Experimental, Illicit
4-MethoxyamphetamineThe therapeutic efficacy of 4-Methoxyamphetamine can be decreased when used in combination with Mianserin.Experimental, Illicit
7-NitroindazoleThe therapeutic efficacy of 7-Nitroindazole can be decreased when used in combination with Mianserin.Experimental
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the neurotoxic activities of Mianserin.Experimental
AbirateroneThe serum concentration of Mianserin can be increased when it is combined with Abiraterone.Approved
AcetazolamideThe therapeutic efficacy of Acetazolamide can be decreased when used in combination with Mianserin.Approved, Vet Approved
AclidiniumMianserin may increase the anticholinergic activities of Aclidinium.Approved
AgmatineThe therapeutic efficacy of Agmatine can be decreased when used in combination with Mianserin.Experimental, Investigational
AlcuroniumMianserin may increase the anticholinergic activities of Alcuronium.Experimental
AmiodaroneThe metabolism of Mianserin can be decreased when combined with Amiodarone.Approved, Investigational
AmobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.Approved, Illicit
AmphetamineAmphetamine may decrease the sedative activities of Mianserin.Approved, Illicit
Anisotropine MethylbromideMianserin may increase the anticholinergic activities of Anisotropine Methylbromide.Approved
Anthranilic acidThe therapeutic efficacy of Anthranilic acid can be decreased when used in combination with Mianserin.Experimental
ApomorphineThe therapeutic efficacy of Apomorphine can be decreased when used in combination with Mianserin.Approved, Investigational
ApraclonidineThe therapeutic efficacy of Apraclonidine can be decreased when used in combination with Mianserin.Approved
AprepitantThe serum concentration of Mianserin can be increased when it is combined with Aprepitant.Approved, Investigational
ArtemetherThe metabolism of Mianserin can be decreased when combined with Artemether.Approved
AtazanavirThe metabolism of Mianserin can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Mianserin can be decreased when combined with Atomoxetine.Approved
AtracuriumMianserin may increase the anticholinergic activities of Atracurium.Experimental, Investigational
Atracurium besylateMianserin may increase the anticholinergic activities of Atracurium besylate.Approved
AtropineMianserin may increase the anticholinergic activities of Atropine.Approved, Vet Approved
AzithromycinThe metabolism of Mianserin can be decreased when combined with Azithromycin.Approved
BarbexacloneThe therapeutic efficacy of Barbexaclone can be decreased when used in combination with Mianserin.Experimental
BarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Barbital.Illicit
BeclamideThe therapeutic efficacy of Beclamide can be decreased when used in combination with Mianserin.Experimental
BenactyzineMianserin may increase the anticholinergic activities of Benactyzine.Withdrawn
BenmoxinBenmoxin may increase the neurotoxic activities of Mianserin.Withdrawn
BenzatropineMianserin may increase the anticholinergic activities of Benzatropine.Approved
BenzphetamineThe therapeutic efficacy of Benzphetamine can be decreased when used in combination with Mianserin.Approved, Illicit
Benzylpenicilloyl PolylysineMianserin may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Betahistine can be decreased when used in combination with Mianserin.Approved
BetaxololThe metabolism of Mianserin can be decreased when combined with Betaxolol.Approved
BethanidineThe therapeutic efficacy of Bethanidine can be decreased when used in combination with Mianserin.Approved
BiperidenMianserin may increase the anticholinergic activities of Biperiden.Approved, Investigational
BoceprevirThe metabolism of Mianserin can be decreased when combined with Boceprevir.Approved, Withdrawn
BornaprineMianserin may increase the anticholinergic activities of Bornaprine.Experimental
BortezomibThe metabolism of Mianserin can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Mianserin can be decreased when it is combined with Bosentan.Approved, Investigational
BrimonidineThe therapeutic efficacy of Brimonidine can be decreased when used in combination with Mianserin.Approved
BrivaracetamThe therapeutic efficacy of Brivaracetam can be decreased when used in combination with Mianserin.Approved, Investigational
BrofaromineBrofaromine may increase the neurotoxic activities of Mianserin.Experimental
BromocriptineThe therapeutic efficacy of Bromocriptine can be decreased when used in combination with Mianserin.Approved, Investigational
BupropionThe metabolism of Mianserin can be decreased when combined with Bupropion.Approved
CaffeineThe metabolism of Mianserin can be decreased when combined with Caffeine.Approved
CarbamazepineThe therapeutic efficacy of Carbamazepine can be decreased when used in combination with Mianserin.Approved, Investigational
CarisbamateThe therapeutic efficacy of Carisbamate can be decreased when used in combination with Mianserin.Investigational
CaroxazoneCaroxazone may increase the neurotoxic activities of Mianserin.Withdrawn
CelecoxibThe metabolism of Mianserin can be decreased when combined with Celecoxib.Approved, Investigational
CeritinibThe serum concentration of Mianserin can be increased when it is combined with Ceritinib.Approved
ChloroquineThe metabolism of Mianserin can be decreased when combined with Chloroquine.Approved, Vet Approved
ChlorphenoxamineMianserin may increase the anticholinergic activities of Chlorphenoxamine.Withdrawn
ChlorphentermineChlorphentermine may decrease the sedative activities of Mianserin.Illicit, Withdrawn
ChlorpromazineThe metabolism of Mianserin can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Mianserin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Mianserin can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Mianserin can be decreased when combined with Cinacalcet.Approved
CitalopramThe metabolism of Mianserin can be decreased when combined with Citalopram.Approved
ClarithromycinThe metabolism of Mianserin can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Mianserin can be decreased when combined with Clemastine.Approved
ClobazamThe therapeutic efficacy of Clobazam can be decreased when used in combination with Mianserin.Approved, Illicit
clomethiazoleThe therapeutic efficacy of clomethiazole can be decreased when used in combination with Mianserin.Investigational
ClomipramineThe metabolism of Mianserin can be decreased when combined with Clomipramine.Approved, Vet Approved
ClonazepamThe therapeutic efficacy of Clonazepam can be decreased when used in combination with Mianserin.Approved, Illicit
ClonidineThe therapeutic efficacy of Clonidine can be decreased when used in combination with Mianserin.Approved
ClopidogrelThe metabolism of Mianserin can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClorazepateThe therapeutic efficacy of Clorazepate can be decreased when used in combination with Mianserin.Approved, Illicit
ClotrimazoleThe metabolism of Mianserin can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Mianserin can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Mianserin can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Mianserin can be decreased when combined with Cocaine.Approved, Illicit
ConivaptanThe serum concentration of Mianserin can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Mianserin can be decreased when combined with Crizotinib.Approved
CyclopentolateMianserin may increase the anticholinergic activities of Cyclopentolate.Approved
CyclosporineThe metabolism of Mianserin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
Cyproterone acetateThe serum concentration of Mianserin can be decreased when it is combined with Cyproterone acetate.Approved, Investigational
DabrafenibThe serum concentration of Mianserin can be decreased when it is combined with Dabrafenib.Approved
DarifenacinMianserin may increase the anticholinergic activities of Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Mianserin can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Mianserin can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Mianserin can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Mianserin can be decreased when combined with Delavirdine.Approved
DelorazepamThe therapeutic efficacy of Delorazepam can be decreased when used in combination with Mianserin.Approved, Illicit, Investigational
DeramciclaneThe therapeutic efficacy of Deramciclane can be decreased when used in combination with Mianserin.Investigational
DesipramineThe metabolism of Mianserin can be decreased when combined with Desipramine.Approved
DesloratadineMianserin may increase the anticholinergic activities of Desloratadine.Approved, Investigational
DexetimideMianserin may increase the anticholinergic activities of Dexetimide.Withdrawn
DexmedetomidineThe therapeutic efficacy of Dexmedetomidine can be decreased when used in combination with Mianserin.Approved, Vet Approved
DextroamphetamineDextroamphetamine may decrease the sedative activities of Mianserin.Approved, Illicit
DiazepamThe therapeutic efficacy of Diazepam can be decreased when used in combination with Mianserin.Approved, Illicit, Vet Approved
DicyclomineMianserin may increase the anticholinergic activities of Dicyclomine.Approved
DiethylpropionDiethylpropion may decrease the sedative activities of Mianserin.Approved, Illicit
DihydroergotamineThe therapeutic efficacy of Dihydroergotamine can be decreased when used in combination with Mianserin.Approved
DiltiazemThe metabolism of Mianserin can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Mianserin can be decreased when combined with Diphenhydramine.Approved
DipivefrinThe therapeutic efficacy of Dipivefrin can be decreased when used in combination with Mianserin.Approved
DoramectinThe therapeutic efficacy of Doramectin can be decreased when used in combination with Mianserin.Vet Approved
DosulepinThe metabolism of Mianserin can be decreased when combined with Dosulepin.Approved
DoxorubicinThe metabolism of Mianserin can be decreased when combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Mianserin can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe metabolism of Mianserin can be decreased when combined with Dronedarone.Approved
DroxidopaThe therapeutic efficacy of Droxidopa can be decreased when used in combination with Mianserin.Approved, Investigational
DuloxetineThe metabolism of Mianserin can be decreased when combined with Duloxetine.Approved
EliglustatThe metabolism of Mianserin can be decreased when combined with Eliglustat.Approved
EmeproniumMianserin may increase the anticholinergic activities of Emepronium.Experimental
EnzalutamideThe serum concentration of Mianserin can be decreased when it is combined with Enzalutamide.Approved
EperisoneThe therapeutic efficacy of Eperisone can be decreased when used in combination with Mianserin.Approved, Investigational
EphedraThe therapeutic efficacy of Ephedra can be decreased when used in combination with Mianserin.Approved, Nutraceutical, Withdrawn
EpinephrineThe therapeutic efficacy of Epinephrine can be decreased when used in combination with Mianserin.Approved, Vet Approved
ErgotamineThe therapeutic efficacy of Ergotamine can be decreased when used in combination with Mianserin.Approved
ErythromycinThe metabolism of Mianserin can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Mianserin.Approved
EstazolamThe therapeutic efficacy of Estazolam can be decreased when used in combination with Mianserin.Approved, Illicit
EtanautineMianserin may increase the anticholinergic activities of Etanautine.Experimental
EthadioneThe therapeutic efficacy of Ethadione can be decreased when used in combination with Mianserin.Experimental
EthopropazineMianserin may increase the anticholinergic activities of Ethopropazine.Approved
EthosuximideThe therapeutic efficacy of Ethosuximide can be decreased when used in combination with Mianserin.Approved
EthotoinThe therapeutic efficacy of Ethotoin can be decreased when used in combination with Mianserin.Approved
EtiracetamThe therapeutic efficacy of Etiracetam can be decreased when used in combination with Mianserin.Investigational
EtomidateThe therapeutic efficacy of Etomidate can be decreased when used in combination with Mianserin.Approved
EtybenzatropineMianserin may increase the anticholinergic activities of Etybenzatropine.Experimental
EzogabineThe therapeutic efficacy of Ezogabine can be decreased when used in combination with Mianserin.Approved
FelbamateThe therapeutic efficacy of Felbamate can be decreased when used in combination with Mianserin.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Mianserin.Approved
FluconazoleThe metabolism of Mianserin can be decreased when combined with Fluconazole.Approved
FludiazepamThe therapeutic efficacy of Fludiazepam can be decreased when used in combination with Mianserin.Approved, Illicit
FlunarizineThe therapeutic efficacy of Flunarizine can be decreased when used in combination with Mianserin.Approved
FluoxetineThe metabolism of Mianserin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe metabolism of Mianserin can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Mianserin can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Mianserin can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mianserin.Approved
FurazolidoneFurazolidone may increase the neurotoxic activities of Mianserin.Approved, Investigational, Vet Approved
Fusidic AcidThe serum concentration of Mianserin can be increased when it is combined with Fusidic Acid.Approved
GabapentinThe therapeutic efficacy of Gabapentin can be decreased when used in combination with Mianserin.Approved, Investigational
GaboxadolThe therapeutic efficacy of Gaboxadol can be decreased when used in combination with Mianserin.Investigational
GallamineMianserin may increase the anticholinergic activities of Gallamine.Experimental
Gallamine TriethiodideMianserin may increase the anticholinergic activities of Gallamine Triethiodide.Approved
GepefrineGepefrine may decrease the sedative activities of Mianserin.Experimental
GlycopyrroniumMianserin may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
GuanabenzThe therapeutic efficacy of Guanabenz can be decreased when used in combination with Mianserin.Approved, Investigational
GuanfacineThe therapeutic efficacy of Guanfacine can be decreased when used in combination with Mianserin.Approved, Investigational
HaloperidolThe metabolism of Mianserin can be decreased when combined with Haloperidol.Approved
HarmalineHarmaline may increase the neurotoxic activities of Mianserin.Experimental
HexamethoniumMianserin may increase the anticholinergic activities of Hexamethonium.Experimental
HexobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Hexobarbital.Approved
HomatropineMianserin may increase the anticholinergic activities of Homatropine.Approved
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Mianserin.Approved, Investigational
HydracarbazineHydracarbazine may increase the neurotoxic activities of Mianserin.Experimental
HydroxyamphetamineHydroxyamphetamine may decrease the sedative activities of Mianserin.Approved
HyoscyamineMianserin may increase the anticholinergic activities of Hyoscyamine.Approved
IdelalisibThe serum concentration of Mianserin can be increased when it is combined with Idelalisib.Approved
IfenprodilThe therapeutic efficacy of Ifenprodil can be decreased when used in combination with Mianserin.Approved, Investigational, Withdrawn
ImatinibThe metabolism of Mianserin can be decreased when combined with Imatinib.Approved
ImipramineThe metabolism of Mianserin can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Mianserin can be decreased when combined with Indinavir.Approved
Iofetamine I-123Iofetamine I-123 may decrease the sedative activities of Mianserin.Approved
Ipratropium bromideMianserin may increase the anticholinergic activities of Ipratropium bromide.Approved
IproclozideIproclozide may increase the neurotoxic activities of Mianserin.Withdrawn
IproniazidIproniazid may increase the neurotoxic activities of Mianserin.Withdrawn
IsavuconazoniumThe metabolism of Mianserin can be decreased when combined with Isavuconazonium.Approved, Investigational
IsocarboxazidIsocarboxazid may increase the neurotoxic activities of Mianserin.Approved
IsoniazidThe metabolism of Mianserin can be decreased when combined with Isoniazid.Approved
IsradipineThe metabolism of Mianserin can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Mianserin can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Mianserin can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe metabolism of Mianserin can be decreased when combined with Ketoconazole.Approved, Investigational
LacosamideThe therapeutic efficacy of Lacosamide can be decreased when used in combination with Mianserin.Approved
LamotrigineThe therapeutic efficacy of Lamotrigine can be decreased when used in combination with Mianserin.Approved, Investigational
LevetiracetamThe therapeutic efficacy of Levetiracetam can be decreased when used in combination with Mianserin.Approved, Investigational
LevonordefrinThe therapeutic efficacy of Levonordefrin can be decreased when used in combination with Mianserin.Approved
LidocaineThe metabolism of Mianserin can be decreased when combined with Lidocaine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Mianserin.Approved, Investigational
LobeglitazoneThe metabolism of Mianserin can be decreased when combined with Lobeglitazone.Approved, Investigational
LofexidineThe therapeutic efficacy of Lofexidine can be decreased when used in combination with Mianserin.Approved, Investigational
LopinavirThe metabolism of Mianserin can be decreased when combined with Lopinavir.Approved
LorazepamThe therapeutic efficacy of Lorazepam can be decreased when used in combination with Mianserin.Approved
LorcaserinThe metabolism of Mianserin can be decreased when combined with Lorcaserin.Approved
LovastatinThe metabolism of Mianserin can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Mianserin can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Mianserin can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Mianserin can be decreased when combined with Lumefantrine.Approved
Magnesium SulfateThe therapeutic efficacy of Magnesium Sulfate can be decreased when used in combination with Mianserin.Approved, Vet Approved
ManidipineThe metabolism of Mianserin can be decreased when combined with Manidipine.Approved, Investigational
MazaticolMianserin may increase the anticholinergic activities of Mazaticol.Experimental
MebanazineMebanazine may increase the neurotoxic activities of Mianserin.Withdrawn
MebeverineThe therapeutic efficacy of Mebeverine can be decreased when used in combination with Mianserin.Investigational
MecamylamineMianserin may increase the anticholinergic activities of Mecamylamine.Approved
MedazepamThe therapeutic efficacy of Medazepam can be decreased when used in combination with Mianserin.Experimental
MephedroneMephedrone may decrease the sedative activities of Mianserin.Investigational
MephentermineMephentermine may decrease the sedative activities of Mianserin.Approved
MephenytoinThe therapeutic efficacy of Mephenytoin can be decreased when used in combination with Mianserin.Investigational, Withdrawn
MeprobamateThe therapeutic efficacy of Meprobamate can be decreased when used in combination with Mianserin.Approved, Illicit
MethadoneThe metabolism of Mianserin can be decreased when combined with Methadone.Approved
MethamphetamineThe therapeutic efficacy of Methamphetamine can be decreased when used in combination with Mianserin.Approved, Illicit
MethanthelineMianserin may increase the anticholinergic activities of Methantheline.Approved, Investigational
MetharbitalThe therapeutic efficacy of Metharbital can be decreased when used in combination with Mianserin.Withdrawn
MethohexitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Methohexital.Approved
MethotrimeprazineThe metabolism of Mianserin can be decreased when combined with Methotrimeprazine.Approved
MethoxyphenamineMethoxyphenamine may decrease the sedative activities of Mianserin.Experimental
MethsuximideThe therapeutic efficacy of Methsuximide can be decreased when used in combination with Mianserin.Approved
Methylene blueMethylene blue may increase the neurotoxic activities of Mianserin.Approved, Investigational
MethylphenobarbitalThe therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Mianserin.Approved
MetixeneMianserin may increase the anticholinergic activities of Metixene.Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Mianserin.Approved, Investigational
MexiletineThe metabolism of Mianserin can be decreased when combined with Mexiletine.Approved
Midomafetamine3,4-Methylenedioxymethamphetamine may decrease the sedative activities of Mianserin.Experimental, Illicit, Investigational
MidostaurinThe metabolism of Mianserin can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Mianserin can be increased when it is combined with Mifepristone.Approved, Investigational
MinaprineMinaprine may increase the neurotoxic activities of Mianserin.Approved
MirabegronThe metabolism of Mianserin can be decreased when combined with Mirabegron.Approved
MitotaneThe serum concentration of Mianserin can be decreased when it is combined with Mitotane.Approved
MK-212The therapeutic efficacy of MK-212 can be decreased when used in combination with Mianserin.Investigational
MMDAMMDA may decrease the sedative activities of Mianserin.Experimental, Illicit
MoclobemideMoclobemide may increase the neurotoxic activities of Mianserin.Approved
MoxonidineThe therapeutic efficacy of Moxonidine can be decreased when used in combination with Mianserin.Approved, Investigational
NaphazolineThe therapeutic efficacy of Naphazoline can be decreased when used in combination with Mianserin.Approved
NefazodoneThe metabolism of Mianserin can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Mianserin can be decreased when combined with Nelfinavir.Approved
NeocitrullamonThe therapeutic efficacy of Neocitrullamon can be decreased when used in combination with Mianserin.Experimental
NetupitantThe serum concentration of Mianserin can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Mianserin can be increased when combined with Nevirapine.Approved
NialamideNialamide may increase the neurotoxic activities of Mianserin.Withdrawn
NicardipineThe metabolism of Mianserin can be decreased when combined with Nicardipine.Approved
NilotinibThe metabolism of Mianserin can be decreased when combined with Nilotinib.Approved, Investigational
NitrazepamThe therapeutic efficacy of Nitrazepam can be decreased when used in combination with Mianserin.Approved
NorepinephrineThe therapeutic efficacy of Norepinephrine can be decreased when used in combination with Mianserin.Approved
OctamoxinOctamoxin may increase the neurotoxic activities of Mianserin.Withdrawn
OlaparibThe metabolism of Mianserin can be decreased when combined with Olaparib.Approved
OrphenadrineMianserin may increase the anticholinergic activities of Orphenadrine.Approved
OsimertinibThe serum concentration of Mianserin can be increased when it is combined with Osimertinib.Approved
OtiloniumMianserin may increase the anticholinergic activities of Otilonium.Experimental, Investigational
OxcarbazepineThe therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mianserin.Approved
OxitropiumMianserin may increase the anticholinergic activities of Oxitropium.Investigational
OxybutyninMianserin may increase the anticholinergic activities of Oxybutynin.Approved, Investigational
OxymetazolineThe therapeutic efficacy of Oxymetazoline can be decreased when used in combination with Mianserin.Approved
OxyphenoniumMianserin may increase the anticholinergic activities of Oxyphenonium.Approved
PalbociclibThe serum concentration of Mianserin can be increased when it is combined with Palbociclib.Approved
PaliperidoneThe therapeutic efficacy of Paliperidone can be decreased when used in combination with Mianserin.Approved
PancuroniumMianserin may increase the anticholinergic activities of Pancuronium.Approved
PanobinostatThe serum concentration of Mianserin can be increased when it is combined with Panobinostat.Approved, Investigational
ParaldehydeThe therapeutic efficacy of Paraldehyde can be decreased when used in combination with Mianserin.Approved, Investigational
ParamethadioneThe therapeutic efficacy of Paramethadione can be decreased when used in combination with Mianserin.Approved
PargylinePargyline may increase the neurotoxic activities of Mianserin.Approved
ParoxetineThe metabolism of Mianserin can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Mianserin can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.Approved, Vet Approved
PentoliniumMianserin may increase the anticholinergic activities of Pentolinium.Approved
PerampanelThe therapeutic efficacy of Perampanel can be decreased when used in combination with Mianserin.Approved
PergolideThe therapeutic efficacy of Pergolide can be decreased when used in combination with Mianserin.Approved, Investigational, Vet Approved, Withdrawn
PhenacemideThe therapeutic efficacy of Phenacemide can be decreased when used in combination with Mianserin.Approved
PhenelzinePhenelzine may increase the neurotoxic activities of Mianserin.Approved
PheneturideThe therapeutic efficacy of Pheneturide can be decreased when used in combination with Mianserin.Experimental
PhenglutarimideMianserin may increase the anticholinergic activities of Phenglutarimide.Experimental
PhenibutThe therapeutic efficacy of Phenibut can be decreased when used in combination with Mianserin.Experimental
PheniprazinePheniprazine may increase the neurotoxic activities of Mianserin.Withdrawn
PhenobarbitalThe therapeutic efficacy of Phenobarbital can be decreased when used in combination with Mianserin.Approved
PhenoxypropazinePhenoxypropazine may increase the neurotoxic activities of Mianserin.Withdrawn
PhensuximideThe therapeutic efficacy of Phensuximide can be decreased when used in combination with Mianserin.Approved
PhenterminePhentermine may decrease the sedative activities of Mianserin.Approved, Illicit
PhenylpropanolamineThe therapeutic efficacy of Phenylpropanolamine can be decreased when used in combination with Mianserin.Approved, Vet Approved, Withdrawn
PhenytoinThe therapeutic efficacy of Phenytoin can be decreased when used in combination with Mianserin.Approved, Vet Approved
PipecuroniumMianserin may increase the anticholinergic activities of Pipecuronium.Approved
PirenzepineMianserin may increase the anticholinergic activities of Pirenzepine.Approved
PirlindolePirlindole may increase the neurotoxic activities of Mianserin.Approved
PivhydrazinePivhydrazine may increase the neurotoxic activities of Mianserin.Withdrawn
PosaconazoleThe metabolism of Mianserin can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PregabalinThe therapeutic efficacy of Pregabalin can be decreased when used in combination with Mianserin.Approved, Illicit, Investigational
PrimidoneThe therapeutic efficacy of Primidone can be decreased when used in combination with Mianserin.Approved, Vet Approved
ProcyclidineMianserin may increase the anticholinergic activities of Procyclidine.Approved
ProgabideThe therapeutic efficacy of Progabide can be decreased when used in combination with Mianserin.Approved, Investigational
PromazineThe metabolism of Mianserin can be decreased when combined with Promazine.Approved, Vet Approved
PropanthelineMianserin may increase the anticholinergic activities of Propantheline.Approved
PropiverineMianserin may increase the anticholinergic activities of Propiverine.Approved, Investigational
PseudoephedrineThe therapeutic efficacy of Pseudoephedrine can be decreased when used in combination with Mianserin.Approved
QuazepamThe serum concentration of Mianserin can be increased when it is combined with Quazepam.Approved, Illicit
QuinidineMianserin may increase the anticholinergic activities of Quinidine.Approved
QuinineThe metabolism of Mianserin can be decreased when combined with Quinine.Approved
RanolazineThe metabolism of Mianserin can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineRasagiline may increase the neurotoxic activities of Mianserin.Approved
remacemideThe therapeutic efficacy of remacemide can be decreased when used in combination with Mianserin.Investigational
RifabutinThe metabolism of Mianserin can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Mianserin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Mianserin can be increased when combined with Rifapentine.Approved
RiluzoleThe therapeutic efficacy of Riluzole can be decreased when used in combination with Mianserin.Approved, Investigational
RisperidoneThe therapeutic efficacy of Risperidone can be decreased when used in combination with Mianserin.Approved, Investigational
RitobegronRitobegron may decrease the sedative activities of Mianserin.Investigational
RitonavirThe metabolism of Mianserin can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Mianserin can be decreased when combined with Rolapitant.Approved
RopiniroleThe therapeutic efficacy of Ropinirole can be decreased when used in combination with Mianserin.Approved, Investigational
RufinamideThe therapeutic efficacy of Rufinamide can be decreased when used in combination with Mianserin.Approved
SafrazineSafrazine may increase the neurotoxic activities of Mianserin.Withdrawn
SaquinavirThe metabolism of Mianserin can be decreased when combined with Saquinavir.Approved, Investigational
ScopolamineMianserin may increase the anticholinergic activities of Scopolamine.Approved
Scopolamine butylbromideMianserin may increase the anticholinergic activities of Scopolamine butylbromide.Approved, Vet Approved
SecobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Secobarbital.Approved, Vet Approved
SelegilineSelegiline may increase the neurotoxic activities of Mianserin.Approved, Investigational, Vet Approved
SertralineThe metabolism of Mianserin can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Mianserin can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Mianserin can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Mianserin can be increased when it is combined with Simeprevir.Approved
SolifenacinMianserin may increase the anticholinergic activities of Solifenacin.Approved
SorafenibThe metabolism of Mianserin can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Mianserin can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
StiripentolThe serum concentration of Mianserin can be increased when it is combined with Stiripentol.Approved
SulfisoxazoleThe metabolism of Mianserin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulthiameThe therapeutic efficacy of Sulthiame can be decreased when used in combination with Mianserin.Experimental
TelaprevirThe metabolism of Mianserin can be decreased when combined with Telaprevir.Approved, Withdrawn
TelithromycinThe metabolism of Mianserin can be decreased when combined with Telithromycin.Approved
Tenofovir disoproxilThe metabolism of Mianserin can be decreased when combined with Tenofovir disoproxil.Approved, Investigational
TerbinafineThe metabolism of Mianserin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TeriflunomideThe serum concentration of Mianserin can be decreased when it is combined with Teriflunomide.Approved
TheophyllineThe metabolism of Mianserin can be decreased when combined with Theophylline.Approved
ThiamylalMianserin may increase the central nervous system depressant (CNS depressant) activities of Thiamylal.Approved, Vet Approved
ThiopentalThe therapeutic efficacy of Thiopental can be decreased when used in combination with Mianserin.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Mianserin.Approved, Withdrawn
ThiotepaThe metabolism of Mianserin can be decreased when combined with Thiotepa.Approved
TiagabineThe therapeutic efficacy of Tiagabine can be decreased when used in combination with Mianserin.Approved
TiclopidineThe metabolism of Mianserin can be decreased when combined with Ticlopidine.Approved
TiletamineThe therapeutic efficacy of Tiletamine can be decreased when used in combination with Mianserin.Vet Approved
TiotropiumMianserin may increase the anticholinergic activities of Tiotropium.Approved
TipranavirThe metabolism of Mianserin can be decreased when combined with Tipranavir.Approved, Investigational
TocilizumabThe serum concentration of Mianserin can be decreased when it is combined with Tocilizumab.Approved
ToloxatoneToloxatone may increase the neurotoxic activities of Mianserin.Approved
TolterodineMianserin may increase the anticholinergic activities of Tolterodine.Approved, Investigational
TopiramateThe therapeutic efficacy of Topiramate can be decreased when used in combination with Mianserin.Approved
tramiprosateThe therapeutic efficacy of tramiprosate can be decreased when used in combination with Mianserin.Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the neurotoxic activities of Mianserin.Experimental
TranylcypromineTranylcypromine may increase the neurotoxic activities of Mianserin.Approved
TrihexyphenidylMianserin may increase the anticholinergic activities of Trihexyphenidyl.Approved
TrimethadioneThe therapeutic efficacy of Trimethadione can be decreased when used in combination with Mianserin.Approved
TrimethaphanMianserin may increase the anticholinergic activities of Trimethaphan.Approved, Investigational
TropatepineMianserin may increase the anticholinergic activities of Tropatepine.Experimental
TropicamideMianserin may increase the anticholinergic activities of Tropicamide.Approved
TrospiumMianserin may increase the anticholinergic activities of Trospium.Approved
TubocurarineMianserin may increase the anticholinergic activities of Tubocurarine.Approved
Valproic AcidThe therapeutic efficacy of Valproic Acid can be decreased when used in combination with Mianserin.Approved, Investigational
ValpromideThe therapeutic efficacy of Valpromide can be decreased when used in combination with Mianserin.Experimental
VecuroniumMianserin may increase the anticholinergic activities of Vecuronium.Approved
VemurafenibThe serum concentration of Mianserin can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe metabolism of Mianserin can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Mianserin can be decreased when combined with Verapamil.Approved
VigabatrinThe therapeutic efficacy of Vigabatrin can be decreased when used in combination with Mianserin.Approved
VinpocetineThe therapeutic efficacy of Vinpocetine can be decreased when used in combination with Mianserin.Investigational
VoriconazoleThe metabolism of Mianserin can be decreased when combined with Voriconazole.Approved, Investigational
XylometazolineThe therapeutic efficacy of Xylometazoline can be decreased when used in combination with Mianserin.Approved
ZaleplonThe therapeutic efficacy of Zaleplon can be decreased when used in combination with Mianserin.Approved, Illicit, Investigational
ZiprasidoneThe metabolism of Mianserin can be decreased when combined with Ziprasidone.Approved
ZonisamideThe therapeutic efficacy of Zonisamide can be decreased when used in combination with Mianserin.Approved, Investigational
ZucapsaicinThe metabolism of Mianserin can be decreased when combined with Zucapsaicin.Approved
Food Interactions
Not Available

References

General References
  1. Koyama E, Chiba K, Tani M, Ishizaki T: Identification of human cytochrome P450 isoforms involved in the stereoselective metabolism of mianserin enantiomers. J Pharmacol Exp Ther. 1996 Jul;278(1):21-30. [PubMed:8764331]
  2. de Boer TH, Nefkens F, van Helvoirt A, van Delft AM: Differences in modulation of noradrenergic and serotonergic transmission by the alpha-2 adrenoceptor antagonists, mirtazapine, mianserin and idazoxan. J Pharmacol Exp Ther. 1996 May;277(2):852-60. [PubMed:8627567]
  3. Kelder J, Funke C, De Boer T, Delbressine L, Leysen D, Nickolson V: A comparison of the physicochemical and biological properties of mirtazapine and mianserin. J Pharm Pharmacol. 1997 Apr;49(4):403-11. [PubMed:9232538]
External Links
Human Metabolome Database
HMDB15620
PubChem Compound
4184
PubChem Substance
46508096
ChemSpider
4040
ChEBI
51137
ChEMBL
CHEMBL6437
Therapeutic Targets Database
DAP000293
PharmGKB
PA134687937
IUPHAR
135
Guide to Pharmacology
GtP Drug Page
Wikipedia
Mianserin
ATC Codes
N06AX03 — Mianserin
MSDS
Download (77.9 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3TerminatedTreatmentAnxiety Disorders / Dementias / Depressive State / Psychosomatic Disorders / Schizophrenic Disorders1
4RecruitingTreatmentDepressive State / Post Traumatic Stress Disorder (PTSD)1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.232 mg/mLALOGPS
logP3.52ALOGPS
logP3.83ChemAxon
logS-3.1ALOGPS
pKa (Strongest Basic)6.92ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area6.48 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity84.5 m3·mol-1ChemAxon
Polarizability30.76 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9703
Blood Brain Barrier+0.9926
Caco-2 permeable+0.8098
P-glycoprotein substrateSubstrate0.8676
P-glycoprotein inhibitor IInhibitor0.8198
P-glycoprotein inhibitor IINon-inhibitor0.9067
Renal organic cation transporterInhibitor0.7953
CYP450 2C9 substrateNon-substrate0.8269
CYP450 2D6 substrateSubstrate0.895
CYP450 3A4 substrateNon-substrate0.5
CYP450 1A2 substrateInhibitor0.8218
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorInhibitor0.8932
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorNon-inhibitor0.8025
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.641
Ames testNon AMES toxic0.8689
CarcinogenicityNon-carcinogens0.9699
BiodegradationNot ready biodegradable0.9972
Rat acute toxicity2.4247 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7801
hERG inhibition (predictor II)Inhibitor0.7369
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0090000000-49135d3660182f98e5f9
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-0090000000-49da9cd1f48c7c59b19c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0aor-4390000000-a6944a5b23139d184375
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4i-8960000000-91b2a10929bb6f8a03e8
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0a4l-6920000000-c2fd706d219cb46dce7c
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-0aou-6910000000-21ad202872a2bb0e4644
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014l-7910000000-e01badcead1453e1b202
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014l-8900000000-a181ec3c5cb717213c41
LC-MS/MS Spectrum - LC-ESI-QFT , positiveLC-MS/MSsplash10-014i-9700000000-0617c8ac60e03f3e0784

Taxonomy

Description
This compound belongs to the class of organic compounds known as dibenzazepines. These are compounds with two benzene rings connected by an azepine ring. Azepine is an unsaturated seven-member heterocycle with one nitrogen atom replacing a carbon atom.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzazepines
Sub Class
Dibenzazepines
Direct Parent
Dibenzazepines
Alternative Parents
Piperazinoazepines / Dialkylarylamines / N-methylpiperazines / Azepines / Aralkylamines / Benzenoids / Trialkylamines / Azacyclic compounds / Organopnictogen compounds / Hydrocarbon derivatives
Substituents
Dibenzazepine / Piperazino-azepine / Dialkylarylamine / Tertiary aliphatic/aromatic amine / Azepine / Aralkylamine / N-alkylpiperazine / N-methylpiperazine / 1,4-diazinane / Piperazine
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
dibenzoazepine (CHEBI:51137)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Thioesterase binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazo...
Gene Name
ADRA2A
Uniprot ID
P08913
Uniprot Name
Alpha-2A adrenergic receptor
Molecular Weight
48956.275 Da
References
  1. Dekeyne A, Millan MJ: Discriminative stimulus properties of the selective and highly potent alpha2-adrenoceptor agonist, S18616, in rats: mediation by the alpha2A subtype, and blockade by the atypical antidepressants, mirtazapine and mianserin. Neuropharmacology. 2006 Sep;51(4):718-26. Epub 2006 Jun 30. [PubMed:16814817]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Virus receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including mescaline, psilocybin, 1-(2,5-dimethoxy-4-iodop...
Gene Name
HTR2A
Uniprot ID
P28223
Uniprot Name
5-hydroxytryptamine receptor 2A
Molecular Weight
52602.58 Da
References
  1. Grinshpoon A, Valevski A, Moskowitz M, Weizman A: Beneficial effect of the addition of the 5-HT 2A/2C and alpha2 antagonist mianserin to ongoing haloperidol treatment in drug-resistant chronically hospitalized schizophrenic patients. Eur Psychiatry. 2000 Sep;15(6):388-90. [PubMed:11004734]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances, including ergot alkaloid derivatives, 1-2,5,-dimethoxy-4-...
Gene Name
HTR2C
Uniprot ID
P28335
Uniprot Name
5-hydroxytryptamine receptor 2C
Molecular Weight
51820.705 Da
References
  1. Grinshpoon A, Valevski A, Moskowitz M, Weizman A: Beneficial effect of the addition of the 5-HT 2A/2C and alpha2 antagonist mianserin to ongoing haloperidol treatment in drug-resistant chronically hospitalized schizophrenic patients. Eur Psychiatry. 2000 Sep;15(6):388-90. [PubMed:11004734]
  2. PDSP Ki Database [Link]
Details
4. Histamine H1 receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamin...
Gene Name
HRH1
Uniprot ID
P35367
Uniprot Name
Histamine H1 receptor
Molecular Weight
55783.61 Da
References
  1. Csaba G, Kovacs P, Pallinger E: Prolonged effect of the tricyclic antidepressant, mianserin on the serotonin and histamine content of young rats' white blood cells and mast cells. A case of late-imprinting. Pharmacol Res. 2003 Nov;48(5):457-60. [PubMed:12967590]
  2. Grinshpoon A, Valevski A, Moskowitz M, Weizman A: Beneficial effect of the addition of the 5-HT 2A/2C and alpha2 antagonist mianserin to ongoing haloperidol treatment in drug-resistant chronically hospitalized schizophrenic patients. Eur Psychiatry. 2000 Sep;15(6):388-90. [PubMed:11004734]
  3. Nowak JZ, Arrang JM, Schwartz JC, Garbarg M: Interaction between mianserin, an antidepressant drug, and central H1- and H2-histamine-receptors: in vitro and in vivo studies and radioreceptor assay. Neuropharmacology. 1983 Mar;22(3):259-66. [PubMed:6302549]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Norepinephrine:sodium symporter activity
Specific Function
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A2
Uniprot ID
P23975
Uniprot Name
Sodium-dependent noradrenaline transporter
Molecular Weight
69331.42 Da
References
  1. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Serotonin:sodium symporter activity
Specific Function
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into t...
Gene Name
SLC6A4
Uniprot ID
P31645
Uniprot Name
Sodium-dependent serotonin transporter
Molecular Weight
70324.165 Da
References
  1. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
Details
7. Histamine H4 receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Histamine receptor activity
Specific Function
The H4 subclass of histamine receptors could mediate the histamine signals in peripheral tissues. Displays a significant level of constitutive activity (spontaneous activity in the absence of agoni...
Gene Name
HRH4
Uniprot ID
Q9H3N8
Uniprot Name
Histamine H4 receptor
Molecular Weight
44495.375 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Blocker
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various drugs and psychoactive substances. Ligand binding causes a conformation change that triggers...
Gene Name
HTR1A
Uniprot ID
P08908
Uniprot Name
5-hydroxytryptamine receptor 1A
Molecular Weight
46106.335 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein homodimerization activity
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins.
Gene Name
ADRA2C
Uniprot ID
P18825
Uniprot Name
Alpha-2C adrenergic receptor
Molecular Weight
49521.585 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various ergot alkaloid derivatives and psychoactive substances. Ligand binding causes a conformation...
Gene Name
HTR2B
Uniprot ID
P41595
Uniprot Name
5-hydroxytryptamine receptor 2B
Molecular Weight
54297.41 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin receptor activity
Specific Function
G-protein coupled receptor for 5-hydroxytryptamine (serotonin). Also functions as a receptor for various alkaloids and psychoactive substances. Ligand binding causes a conformation change that trig...
Gene Name
HTR1F
Uniprot ID
P30939
Uniprot Name
5-hydroxytryptamine receptor 1F
Molecular Weight
41708.505 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Epinephrine binding
Specific Function
Alpha-2 adrenergic receptors mediate the catecholamine-induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine...
Gene Name
ADRA2B
Uniprot ID
P18089
Uniprot Name
Alpha-2B adrenergic receptor
Molecular Weight
49565.8 Da
References
  1. PDSP Ki Database [Link]
Details
13. D(3) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase. Promotes cell proliferation.
Gene Name
DRD3
Uniprot ID
P35462
Uniprot Name
D(3) dopamine receptor
Molecular Weight
44224.335 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Agonist
General Function
Opioid receptor activity
Specific Function
G-protein coupled opioid receptor that functions as receptor for endogenous alpha-neoendorphins and dynorphins, but has low affinity for beta-endorphins. Also functions as receptor for various synt...
Gene Name
OPRK1
Uniprot ID
P41145
Uniprot Name
Kappa-type opioid receptor
Molecular Weight
42644.665 Da
References
  1. Olianas MC, Dedoni S, Onali P: The atypical antidepressant mianserin exhibits agonist activity at kappa-opioid receptors. Br J Pharmacol. 2012 Nov;167(6):1329-41. doi: 10.1111/j.1476-5381.2012.02078.x. [PubMed:22708686]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Monoamine transmembrane transporter activity
Specific Function
Amine transporter. Terminates the action of dopamine by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name
SLC6A3
Uniprot ID
Q01959
Uniprot Name
Sodium-dependent dopamine transporter
Molecular Weight
68494.255 Da
References
  1. Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58. [PubMed:9537821]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR7
Uniprot ID
P34969
Uniprot Name
5-hydroxytryptamine receptor 7
Molecular Weight
53554.43 Da
References
  1. Lucchelli A, Santagostino-Barbone MG, D'Agostino G, Masoero E, Tonini M: The interaction of antidepressant drugs with enteric 5-HT7 receptors. Naunyn Schmiedebergs Arch Pharmacol. 2000 Sep;362(3):284-9. [PubMed:10997731]
  2. PDSP Ki Database [Link]
Details
17. D(2) dopamine receptor
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Potassium channel regulator activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which inhibit adenylyl cyclase.
Gene Name
DRD2
Uniprot ID
P14416
Uniprot Name
D(2) dopamine receptor
Molecular Weight
50618.91 Da
References
  1. Terai M, Hidaka K, Nakamura Y: Comparison of [3H]YM-09151-2 with [3H]spiperone and [3H]raclopride for dopamine d-2 receptor binding to rat striatum. Eur J Pharmacol. 1989 Dec 7;173(2-3):177-82. [PubMed:2576228]
  2. PDSP Ki Database [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
Serotonin receptor activity
Specific Function
This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor ...
Gene Name
HTR6
Uniprot ID
P50406
Uniprot Name
5-hydroxytryptamine receptor 6
Molecular Weight
46953.625 Da
References
  1. PDSP Ki Database [Link]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Protein heterodimerization activity
Specific Function
This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. Its effect is mediated by G(q) and G(11) prot...

Components:
References
  1. PDSP Ki Database [Link]
Kind
Protein group
Organism
Human
Pharmacological action
Unknown
Actions
Binder
General Function
G-protein coupled amine receptor activity
Specific Function
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.

Components:
References
  1. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Rojdmark S, von Bahr C: [Metabolic interaction between psychopharmaceuticals. Probable cause of exacerbation of hypothyroidism according to a case report]. Lakartidningen. 2002 Jun 20;99(25):2854-6. [PubMed:12143142]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Rojdmark S, von Bahr C: [Metabolic interaction between psychopharmaceuticals. Probable cause of exacerbation of hypothyroidism according to a case report]. Lakartidningen. 2002 Jun 20;99(25):2854-6. [PubMed:12143142]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Drug created on November 25, 2007 11:28 / Updated on November 09, 2017 03:53