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Identification
NameMianserin
Accession NumberDB06148
TypeSmall Molecule
GroupsApproved
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
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 KeyInChIKey=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
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
Pharmacology
IndicationFor the treatment of depression.
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.
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
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
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)
Interactions
Drug Interactions
Drug
AcetazolamideThe therapeutic efficacy of Acetazolamide can be decreased when used in combination with Mianserin.
AclidiniumMianserin may increase the anticholinergic activities of Aclidinium.
AmitriptylineMianserin may increase the anticholinergic activities of Amitriptyline.
AmobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Amobarbital.
AmoxapineMianserin may increase the anticholinergic activities of Amoxapine.
ApraclonidineThe therapeutic efficacy of Apraclonidine can be decreased when used in combination with Mianserin.
AtropineMianserin may increase the anticholinergic activities of Atropine.
BenzatropineMianserin may increase the anticholinergic activities of Benzatropine.
BrimonidineThe therapeutic efficacy of Brimonidine can be decreased when used in combination with Mianserin.
BrompheniramineMianserin may increase the anticholinergic activities of Brompheniramine.
ButabarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Butabarbital.
CarbamazepineThe therapeutic efficacy of Carbamazepine can be decreased when used in combination with Mianserin.
CarbinoxamineMianserin may increase the anticholinergic activities of Carbinoxamine.
CetirizineMianserin may increase the anticholinergic activities of Cetirizine.
ChlorphenamineMianserin may increase the anticholinergic activities of Chlorphenamine.
ChlorpromazineMianserin may increase the anticholinergic activities of Chlorpromazine.
ClemastineMianserin may increase the anticholinergic activities of Clemastine.
ClomipramineMianserin may increase the anticholinergic activities of Clomipramine.
ClozapineMianserin may increase the anticholinergic activities of Clozapine.
CyclizineMianserin may increase the anticholinergic activities of Cyclizine.
CyclobenzaprineMianserin may increase the anticholinergic activities of Cyclobenzaprine.
CyclopentolateMianserin may increase the anticholinergic activities of Cyclopentolate.
CyproheptadineMianserin may increase the anticholinergic activities of Cyproheptadine.
DarifenacinMianserin may increase the anticholinergic activities of Darifenacin.
DesipramineMianserin may increase the anticholinergic activities of Desipramine.
DesloratadineMianserin may increase the anticholinergic activities of Desloratadine.
Dexchlorpheniramine maleateMianserin may increase the anticholinergic activities of Dexchlorpheniramine maleate.
DicyclomineMianserin may increase the anticholinergic activities of Dicyclomine.
DimenhydrinateMianserin may increase the anticholinergic activities of Dimenhydrinate.
DiphenhydramineMianserin may increase the anticholinergic activities of Diphenhydramine.
DoxepinMianserin may increase the anticholinergic activities of Doxepin.
DoxylamineMianserin may increase the anticholinergic activities of Doxylamine.
Eslicarbazepine acetateThe therapeutic efficacy of Eslicarbazepine acetate can be decreased when used in combination with Mianserin.
EthosuximideThe therapeutic efficacy of Ethosuximide can be decreased when used in combination with Mianserin.
EthotoinThe therapeutic efficacy of Ethotoin can be decreased when used in combination with Mianserin.
EzogabineThe therapeutic efficacy of Ezogabine can be decreased when used in combination with Mianserin.
FelbamateThe therapeutic efficacy of Felbamate can be decreased when used in combination with Mianserin.
FesoterodineMianserin may increase the anticholinergic activities of Fesoterodine.
FexofenadineMianserin may increase the anticholinergic activities of Fexofenadine.
FlavoxateMianserin may increase the anticholinergic activities of Flavoxate.
FluphenazineMianserin may increase the anticholinergic activities of Fluphenazine.
FosphenytoinThe therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Mianserin.
GabapentinThe therapeutic efficacy of Gabapentin can be decreased when used in combination with Mianserin.
GlycopyrroniumMianserin may increase the anticholinergic activities of Glycopyrrolate.
HaloperidolMianserin may increase the anticholinergic activities of Haloperidol.
HomatropineMianserin may increase the anticholinergic activities of Homatropine.
HydroxyzineMianserin may increase the anticholinergic activities of Hydroxyzine.
HyoscyamineMianserin may increase the anticholinergic activities of Hyoscyamine.
ImipramineMianserin may increase the anticholinergic activities of Imipramine.
Ipratropium bromideMianserin may increase the anticholinergic activities of Ipratropium bromide.
IsocarboxazidIsocarboxazid may increase the neurotoxic activities of Mianserin.
LacosamideThe therapeutic efficacy of Lacosamide can be decreased when used in combination with Mianserin.
LamotrigineThe therapeutic efficacy of Lamotrigine can be decreased when used in combination with Mianserin.
LevetiracetamThe therapeutic efficacy of Levetiracetam can be decreased when used in combination with Mianserin.
LevocabastineMianserin may increase the anticholinergic activities of Levocabastine.
LevocetirizineMianserin may increase the anticholinergic activities of Levocetirizine.
LinezolidLinezolid may increase the neurotoxic activities of Mianserin.
LoratadineMianserin may increase the anticholinergic activities of Loratadine.
LoxapineMianserin may increase the anticholinergic activities of Loxapine.
MaprotilineMianserin may increase the anticholinergic activities of Maprotiline.
MeclizineMianserin may increase the anticholinergic activities of Meclizine.
MepenzolateMianserin may increase the anticholinergic activities of Mepenzolate.
MethohexitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Methohexital.
MethscopolamineMianserin may increase the anticholinergic activities of Methscopolamine.
MethsuximideThe therapeutic efficacy of Methsuximide can be decreased when used in combination with Mianserin.
MoclobemideMoclobemide may increase the neurotoxic activities of Mianserin.
NortriptylineMianserin may increase the anticholinergic activities of Nortriptyline.
OlanzapineMianserin may increase the anticholinergic activities of Olanzapine.
OlopatadineMianserin may increase the anticholinergic activities of Olopatadine.
OxcarbazepineThe therapeutic efficacy of Oxcarbazepine can be decreased when used in combination with Mianserin.
OxybutyninMianserin may increase the anticholinergic activities of Oxybutynin.
PentobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Pentobarbital.
PerphenazineMianserin may increase the anticholinergic activities of Perphenazine.
PhenelzinePhenelzine may increase the neurotoxic activities of Mianserin.
PhenobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Phenobarbital.
PhenytoinThe therapeutic efficacy of Phenytoin can be decreased when used in combination with Mianserin.
PizotifenMianserin may increase the anticholinergic activities of Pizotifen.
PregabalinThe therapeutic efficacy of Pregabalin can be decreased when used in combination with Mianserin.
ProcarbazineProcarbazine may increase the neurotoxic activities of Mianserin.
ProchlorperazineMianserin may increase the anticholinergic activities of Prochlorperazine.
ProcyclidineMianserin may increase the anticholinergic activities of Procyclidine.
PromazineMianserin may increase the anticholinergic activities of Promazine.
PromethazineMianserin may increase the anticholinergic activities of Promethazine.
PropanthelineMianserin may increase the anticholinergic activities of Propantheline.
ProtriptylineMianserin may increase the anticholinergic activities of Protriptyline.
RasagilineRasagiline may increase the neurotoxic activities of Mianserin.
RisperidoneMianserin may increase the anticholinergic activities of Risperidone.
ScopolamineMianserin may increase the anticholinergic activities of Scopolamine.
Scopolamine butylbromideMianserin may increase the anticholinergic activities of Scopolamine butylbromide.
SecobarbitalMianserin may increase the central nervous system depressant (CNS depressant) activities of Secobarbital.
SelegilineSelegiline may increase the neurotoxic activities of Mianserin.
SolifenacinMianserin may increase the anticholinergic activities of Solifenacin.
StiripentolThe therapeutic efficacy of Stiripentol can be decreased when used in combination with Mianserin.
Tedizolid PhosphateTedizolid Phosphate may increase the neurotoxic activities of Mianserin.
ThiothixeneMianserin may increase the anticholinergic activities of Thiothixene.
TiagabineThe therapeutic efficacy of Tiagabine can be decreased when used in combination with Mianserin.
TiotropiumMianserin may increase the anticholinergic activities of Tiotropium.
TolterodineMianserin may increase the anticholinergic activities of Tolterodine.
TopiramateThe therapeutic efficacy of Topiramate can be decreased when used in combination with Mianserin.
TranylcypromineTranylcypromine may increase the neurotoxic activities of Mianserin.
TrifluoperazineMianserin may increase the anticholinergic activities of Trifluoperazine.
TrihexyphenidylMianserin may increase the anticholinergic activities of Trihexyphenidyl.
TrimethobenzamideMianserin may increase the anticholinergic activities of Trimethobenzamide.
TrimipramineMianserin may increase the anticholinergic activities of Trimipramine.
TriprolidineMianserin may increase the anticholinergic activities of Triprolidine.
TrospiumMianserin may increase the anticholinergic activities of Trospium.
UmeclidiniumMianserin may increase the anticholinergic activities of Umeclidinium.
Valproic AcidThe therapeutic efficacy of Valproic Acid can be decreased when used in combination with Mianserin.
VigabatrinThe therapeutic efficacy of Vigabatrin can be decreased when used in combination with Mianserin.
ZonisamideThe therapeutic efficacy of Zonisamide can be decreased when used in combination with Mianserin.
Food InteractionsNot 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