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Identification
NameMianserin
Accession NumberDB06148
TypeSmall Molecule
GroupsApproved
DescriptionA 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
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
BolvidonNot Available
DepnonNot Available
LantanonNot Available
LuminNot Available
NorvalNot Available
TolvonNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Mianserin hydrochloride
ThumbNot applicableDBSALT000957
Categories
UNII250PJI13LM
CAS number24219-97-4
WeightAverage: 264.3648
Monoisotopic: 264.16264865
Chemical FormulaC18H20N2
InChI KeyUEQUQVLFIPOEMF-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
IndicationFor the treatment of depression.
Structured Indications Not Available
PharmacodynamicsMianserin 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 actionMianserin's mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors.
TargetKindPharmacological actionActionsOrganismUniProt ID
Alpha-2A adrenergic receptorProteinunknown
antagonist
HumanP08913 details
5-hydroxytryptamine receptor 2AProteinunknown
antagonist
HumanP28223 details
5-hydroxytryptamine receptor 2CProteinunknown
antagonist
HumanP28335 details
Histamine H1 receptorProteinunknown
antagonist
HumanP35367 details
Sodium-dependent noradrenaline transporterProteinunknown
inhibitor
HumanP23975 details
Sodium-dependent serotonin transporterProteinunknown
inhibitor
HumanP31645 details
Histamine H4 receptorProteinunknown
binder
HumanQ9H3N8 details
5-hydroxytryptamine receptor 1AProteinunknown
blocker
HumanP08908 details
Alpha-2C adrenergic receptorProteinunknown
antagonist
HumanP18825 details
5-hydroxytryptamine receptor 2BProteinunknown
binder
HumanP41595 details
5-hydroxytryptamine receptor 1FProteinunknown
binder
HumanP30939 details
Alpha-2B adrenergic receptorProteinunknown
antagonist
HumanP18089 details
D(3) dopamine receptorProteinunknown
binder
HumanP35462 details
Kappa-type opioid receptorProteinunknown
agonist
HumanP41145 details
Sodium-dependent dopamine transporterProteinunknown
binder
HumanQ01959 details
5-hydroxytryptamine receptor 7Proteinunknown
antagonist
HumanP34969 details
D(2) dopamine receptorProteinunknown
antagonist
HumanP14416 details
5-hydroxytryptamine receptor 6Proteinunknown
binder
HumanP50406 details
Alpha-1 adrenergic receptorProtein groupunknown
antagonist
Humannot applicabledetails
D(1) dopamine receptorProtein groupunknown
binder
Humannot applicabledetails
Related Articles
AbsorptionAbsorbed following oral administration.
Volume of distributionNot Available
Protein binding90%
Metabolism

Hepatic.

Route of eliminationNot Available
Half life10-17 hours
ClearanceNot Available
ToxicityOral rat LD50: 780mg/kg
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2-Aminobenzoic AcidThe therapeutic efficacy of 2-Aminobenzoic Acid can be decreased when used in combination with Mianserin.Experimental
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
3,4-Methylenedioxymethamphetamine3,4-Methylenedioxymethamphetamine 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
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
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
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
BarbexacloneMianserin may increase the central nervous system depressant (CNS depressant) activities of Barbexaclone.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
BexaroteneThe serum concentration of Mianserin can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenMianserin may increase the anticholinergic activities of Biperiden.Approved
BoceprevirThe metabolism of Mianserin can be decreased when combined with Boceprevir.Approved
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.Investigational
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
CppThe therapeutic efficacy of Cpp can be decreased when used in combination with Mianserin.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
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
DexamethasoneThe serum concentration of Mianserin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
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
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
EfavirenzThe serum concentration of Mianserin can be decreased when it is combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Mianserin can be decreased when combined with Eliglustat.Approved
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
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
EtravirineThe serum concentration of Mianserin can be decreased when it is combined with Etravirine.Approved
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, 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
Gallamine TriethiodideMianserin may increase the anticholinergic activities of Gallamine Triethiodide.Approved
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
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
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.Approved
Hydroxyamphetamine hydrobromideHydroxyamphetamine hydrobromide 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, 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
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
LidocaineThe metabolism of Mianserin can be decreased when combined with Lidocaine.Approved, Vet Approved
LisdexamfetamineLisdexamfetamine may decrease the sedative activities of Mianserin.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
MebanazineMebanazine may increase the neurotoxic activities of Mianserin.Withdrawn
MecamylamineMianserin may increase the anticholinergic activities of Mecamylamine.Approved
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
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
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.Investigational
MethylphenobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Methylphenobarbital.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
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
MMDAMMDA may decrease the sedative activities of Mianserin.Experimental, Illicit
MoclobemideMoclobemide may increase the neurotoxic activities of Mianserin.Approved
ModafinilThe serum concentration of Mianserin can be decreased when it is combined with Modafinil.Approved, Investigational
N-butylscopolammonium bromideMianserin may increase the anticholinergic activities of N-butylscopolammonium bromide.Vet Approved
NafcillinThe serum concentration of Mianserin can be decreased when it is combined with Nafcillin.Approved
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
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
NVA237Mianserin may increase the anticholinergic activities of NVA237.Investigational
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
OxcarbazepineThe therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mianserin.Approved
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
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, 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
PheniprazinePheniprazine may increase the neurotoxic activities of Mianserin.Withdrawn
PhenobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.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
PrimidoneMianserin may increase the central nervous system depressant (CNS depressant) activities of Primidone.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.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
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.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
TelithromycinThe metabolism of Mianserin can be decreased when combined with Telithromycin.Approved
TenofovirThe metabolism of Mianserin can be decreased when combined with Tenofovir.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
ThiopentalMianserin may increase the central nervous system depressant (CNS depressant) activities of Thiopental.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Mianserin.Approved
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
TizanidineThe therapeutic efficacy of Tizanidine can be decreased when used in combination with Mianserin.Approved
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
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
UmeclidiniumMianserin may increase the anticholinergic activities of Umeclidinium.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
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
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
ATC CodesN06AX03
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSDownload (77.9 KB)
ADMET
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 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot 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 RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis 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.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzazepines
Sub ClassDibenzazepines
Direct ParentDibenzazepines
Alternative Parents
Substituents
  • Dibenzazepine
  • Piperazino-azepine
  • Dialkylarylamine
  • Aralkylamine
  • N-alkylpiperazine
  • N-methylpiperazine
  • Azepine
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Hydrocarbon derivative
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianser...
Gene Name:
ADRA2A
Uniprot ID:
P08913
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-iodophenyl)-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates...
Gene Name:
HTR2A
Uniprot ID:
P28223
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-iodophenyl-2-aminopropane (DOI) and lysergic acid diethylamide (LSD). Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modul...
Gene Name:
HTR2C
Uniprot ID:
P28335
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]
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 catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system.
Gene Name:
HRH1
Uniprot ID:
P35367
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
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 the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
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 ]
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 agonist).
Gene Name:
HRH4
Uniprot ID:
Q9H3N8
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 signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Beta-arrestin family members inhibit signaling via G pro...
Gene Name:
HTR1A
Uniprot ID:
P08908
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
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 change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors. Beta-arrestin family members inhibit signaling via G proteins ...
Gene Name:
HTR2B
Uniprot ID:
P41595
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 triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase activity.
Gene Name:
HTR1F
Uniprot ID:
P30939
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 > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phent...
Gene Name:
ADRA2B
Uniprot ID:
P18089
Molecular Weight:
49565.8 Da
References
  1. PDSP Ki Database [Link]
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
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 synthetic opioids and for the psychoactive diterpene salvinorin A. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates th...
Gene Name:
OPRK1
Uniprot ID:
P41145
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
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 is mediated by G proteins that stimulate adenylate cyclase.
Gene Name:
HTR7
Uniprot ID:
P34969
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]
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
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 is mediated by G proteins that stimulate adenylate cyclase. It has a high affinity for tricyclic psychotropic drugs (By similarity). Controls pyramidal neurons migration during corticogenesis, through...
Gene Name:
HTR6
Uniprot ID:
P50406
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) proteins. Nuclear ADRA1A-ADRA1B heterooligomers regulate phenylephrine(PE)-stimulated ERK signaling in cardiac myocytes.
Components:
NameUniProt IDDetails
Alpha-1A adrenergic receptorP35348 Details
Alpha-1B adrenergic receptorP35368 Details
Alpha-1D adrenergic receptorP25100 Details
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:
NameUniProt IDDetails
D(1A) dopamine receptorP21728 Details
D(1B) dopamine receptorP21918 Details
References
  1. PDSP Ki Database [Link]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
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 reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
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 ]
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Drug created on November 25, 2007 11:28 / Updated on August 17, 2016 12:24