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Identification
NameThioproperazine
Accession NumberDB01622
TypeSmall Molecule
GroupsApproved
DescriptionThioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property. It is used for the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes. Overdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma. LD50 in mice is 70 mg/kg I.V., 120 mg/kg I.P., 500 mg/kg S.C. and 830 mg/kg P.O.
Structure
Thumb
Synonyms
(Thioproperazine)-2-dimethylsulfamido-(10-(3-1-methylpiperazinyl-4)propyl)-phenothiazine
2-Dimethylsulfamido-(10-(3-1-methylpiperazinyl-4)propyl)-phenothiazine
N,N-Dimethyl-10-[3-(4-methyl-1-piperazinyl)propyl]-10H-phenothiazine-2-sulfonamide
N,N-Dimethyl-10-[3-(4-methyl-1-piperazinyl)propyl]phenothiazine-2-sulfonamide
Thioperazine
Thioproperazin
Thioproperazinum
Tioproferazina
Tioproperazina
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Majeptil Tab 10mgTablet10 mgOralErfa Canada 2012 Inc1962-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MajeptilNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIYJ050AQ56X
CAS number316-81-4
WeightAverage: 446.629
Monoisotopic: 446.181017604
Chemical FormulaC22H30N4O2S2
InChI KeyVZYCZNZBPPHOFY-UHFFFAOYSA-N
InChI
InChI=1S/C22H30N4O2S2/c1-23(2)30(27,28)18-9-10-22-20(17-18)26(19-7-4-5-8-21(19)29-22)12-6-11-25-15-13-24(3)14-16-25/h4-5,7-10,17H,6,11-16H2,1-3H3
IUPAC Name
N,N-dimethyl-10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine-2-sulfonamide
SMILES
CN(C)S(=O)(=O)C1=CC2=C(SC3=CC=CC=C3N2CCCN2CCN(C)CC2)C=C1
Pharmacology
IndicationFor the treatment of all types of acute and chronic schizophrenia, including those which did not respond to the usual neuroleptics; manic syndromes.
Structured Indications
PharmacodynamicsThioproperazine is a potent neuroleptic with antipsychotic properties. Thioproperazine has a marked cataleptic and antiapomorphine activity associated with relatively slight sedative, hypothermic and spasmolytic effects. It is virtually without antiserotonin and hypotensive action and has no antihistaminic property.
Mechanism of actionThioproperazine acts as an antagonist (blocking agent) on different postsysnaptic receptors -on dopaminergic-receptors (subtypes D1, D2, D3 and D4 - different antipsychotic properties on productive and unproductive symptoms), on serotonergic-receptors (5-HT1 and 5-HT2, with anxiolytic, antidepressive and antiaggressive properties as well as an attenuation of extrapypramidal side-effects, but also leading to weight gain, fall in blood pressure, sedation and ejaculation difficulties), on histaminergic-receptors (H1-receptors, sedation, antiemesis, vertigo, fall in blood pressure and weight gain), alpha1/alpha2-receptors (antisympathomimetic properties, lowering of blood pressure, reflex tachycardia, vertigo, sedation, hypersalivation and incontinence as well as sexual dysfunction, but may also attenuate pseudoparkinsonism - controversial) and finally on muscarinic (cholinergic) M1/M2-receptors (causing anticholinergic symptoms like dry mouth, blurred vision, obstipation, difficulty/inability to urinate, sinus tachycardia, ECG-changes and loss of memory, but the anticholinergic action may attenuate extrapyramidal side-effects).
TargetKindPharmacological actionActionsOrganismUniProt ID
D(2) dopamine receptorProteinyes
antagonist
HumanP14416 details
D(1A) dopamine receptorProteinunknown
antagonist
HumanP21728 details
5-hydroxytryptamine receptor 2AProteinyes
antagonist
HumanP28223 details
5-hydroxytryptamine receptor 1AProteinyes
antagonist
HumanP08908 details
Alpha-1A adrenergic receptorProteinyes
antagonist
HumanP35348 details
Alpha-1B adrenergic receptorProteinyes
antagonist
HumanP35368 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityOverdosage may result in severe extrapyramidal symptoms with dysphagia, marked sialorrhea, persistent and rapidly increasing hyperthermia, pulmonary syndrome, state of shock with pallor and profuse sweating, which may be followed by collapse and coma. LD50 in mice is 70 mg/kg I.V., 120 mg/kg I.P., 500 mg/kg S.C. and 830 mg/kg P.O.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
2,5-Dimethoxy-4-ethylamphetamineThioproperazine may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.Experimental, Illicit
3,4-MethylenedioxyamphetamineThioproperazine may decrease the stimulatory activities of 3,4-Methylenedioxyamphetamine.Experimental, Illicit
3,4-MethylenedioxymethamphetamineThioproperazine may decrease the stimulatory activities of 3,4-Methylenedioxymethamphetamine.Experimental, Illicit
4-Bromo-2,5-dimethoxyamphetamineThioproperazine may decrease the stimulatory activities of 4-Bromo-2,5-dimethoxyamphetamine.Experimental, Illicit
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Thioproperazine.Approved, Investigational
AmantadineThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Amantadine.Approved
AmisulprideThe risk or severity of adverse effects can be increased when Thioproperazine is combined with Amisulpride.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Thioproperazine.Approved
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Thioproperazine.Approved
AmphetamineThioproperazine may decrease the stimulatory activities of Amphetamine.Approved, Illicit
ApomorphineThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Apomorphine.Approved, Investigational
BenzphetamineThioproperazine may decrease the stimulatory activities of Benzphetamine.Approved, Illicit
BromocriptineThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Bromocriptine.Approved, Investigational
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Thioproperazine.Approved, Investigational
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Thioproperazine.Approved
ChlorphentermineThioproperazine may decrease the stimulatory activities of Chlorphentermine.Illicit, Withdrawn
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Thioproperazine.Approved
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Thioproperazine.Approved, Vet Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Thioproperazine.Approved
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Thioproperazine.Approved
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Thioproperazine.Approved
DextroamphetamineThioproperazine may decrease the stimulatory activities of Dextroamphetamine.Approved, Illicit
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Thioproperazine.Approved
DiethylpropionThioproperazine may decrease the stimulatory activities of Diethylpropion.Approved, Illicit
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Thioproperazine.Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Thioproperazine.Approved
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Thioproperazine.Approved
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Thioproperazine.Approved, Investigational
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Thioproperazine.Approved
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Thioproperazine.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Thioproperazine.Approved
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Thioproperazine.Approved, Investigational
FentanylThe risk or severity of adverse effects can be increased when Fentanyl is combined with Thioproperazine.Approved, Illicit, Investigational, Vet Approved
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Thioproperazine.Approved, Vet Approved
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Thioproperazine.Approved, Investigational
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Thioproperazine.Approved, Investigational
Hydroxyamphetamine hydrobromideThioproperazine may decrease the stimulatory activities of Hydroxyamphetamine hydrobromide.Approved
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Thioproperazine.Approved
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Thioproperazine.Approved
LevodopaThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Levodopa.Approved
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Thioproperazine.Approved
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Thioproperazine.Approved, Investigational
LisdexamfetamineThioproperazine may decrease the stimulatory activities of Lisdexamfetamine.Approved, Investigational
LithiumLithium may increase the neurotoxic activities of Thioproperazine.Approved
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Thioproperazine.Approved
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Thioproperazine.Approved
MephedroneThioproperazine may decrease the stimulatory activities of Mephedrone.Investigational
MephentermineThioproperazine may decrease the stimulatory activities of Mephentermine.Approved
MequitazineThioproperazine may increase the arrhythmogenic activities of Mequitazine.Approved
MethadoneThe risk or severity of adverse effects can be increased when Methadone is combined with Thioproperazine.Approved
MethamphetamineThioproperazine may decrease the stimulatory activities of Methamphetamine.Approved, Illicit
MethylphenidateThe risk or severity of adverse effects can be increased when Thioproperazine is combined with Methylphenidate.Approved, Investigational
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Thioproperazine.Approved, Investigational
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Thioproperazine.Approved
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Thioproperazine.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Thioproperazine.Approved
MMDAThioproperazine may decrease the stimulatory activities of MMDA.Experimental, Illicit
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Thioproperazine.Approved
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Thioproperazine.Approved, Investigational
NefazodoneThe risk or severity of adverse effects can be increased when Nefazodone is combined with Thioproperazine.Approved, Withdrawn
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Thioproperazine.Approved
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Thioproperazine.Approved, Investigational
PethidineThe risk or severity of adverse effects can be increased when Pethidine is combined with Thioproperazine.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Thioproperazine.Approved
PhentermineThioproperazine may decrease the stimulatory activities of Phentermine.Approved, Illicit
PiribedilThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Piribedil.Investigational
PramipexoleThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Pramipexole.Approved, Investigational
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Thioproperazine.Approved
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Thioproperazine.Approved
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Thioproperazine.Approved
PseudoephedrineThioproperazine may decrease the stimulatory activities of Pseudoephedrine.Approved
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Thioproperazine.Approved
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Thioproperazine.Approved
RitobegronThioproperazine may decrease the stimulatory activities of Ritobegron.Investigational
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Thioproperazine.Approved
RopiniroleThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Ropinirole.Approved, Investigational
RotigotineThe therapeutic efficacy of Thioproperazine can be decreased when used in combination with Rotigotine.Approved
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Thioproperazine.Approved, Investigational, Vet Approved
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Thioproperazine.Approved
SulpirideThe risk or severity of adverse effects can be increased when Thioproperazine is combined with Sulpiride.Approved
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Thioproperazine.Approved, Investigational
TapentadolThe risk or severity of adverse effects can be increased when Tapentadol is combined with Thioproperazine.Approved
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Thioproperazine.Approved
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Thioproperazine.Approved
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Thioproperazine.Approved, Investigational
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Thioproperazine.Approved
TrazodoneThe risk or severity of adverse effects can be increased when Trazodone is combined with Thioproperazine.Approved, Investigational
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Thioproperazine.Approved
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Thioproperazine.Approved
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Thioproperazine.Approved
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Thioproperazine.Approved
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Thioproperazine.Approved, Investigational
Food Interactions
  • Avoid alcohol
  • Take with food to avoid irritation
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN05AB08
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.996
Blood Brain Barrier+0.9629
Caco-2 permeable-0.6568
P-glycoprotein substrateSubstrate0.7908
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.7979
Renal organic cation transporterNon-inhibitor0.5396
CYP450 2C9 substrateNon-substrate0.7704
CYP450 2D6 substrateNon-substrate0.8194
CYP450 3A4 substrateSubstrate0.5366
CYP450 1A2 substrateNon-inhibitor0.8243
CYP450 2C9 inhibitorNon-inhibitor0.8758
CYP450 2D6 inhibitorInhibitor0.6293
CYP450 2C19 inhibitorNon-inhibitor0.7713
CYP450 3A4 inhibitorInhibitor0.6338
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6663
Ames testNon AMES toxic0.7056
CarcinogenicityNon-carcinogens0.8109
BiodegradationNot ready biodegradable0.9934
Rat acute toxicity2.6623 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7265
hERG inhibition (predictor II)Non-inhibitor0.5303
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
TabletOral10 mg
Prices
Unit descriptionCostUnit
Majeptil 10 mg Tablet0.6USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point140 °CPhysProp
Predicted Properties
PropertyValueSource
Water Solubility0.0569 mg/mLALOGPS
logP3.09ALOGPS
logP2.83ChemAxon
logS-3.9ALOGPS
pKa (Strongest Basic)8.36ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area47.1 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity126.95 m3·mol-1ChemAxon
Polarizability49.62 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (11 KB)
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 phenothiazines. These are polycyclic aromatic compounds containing a phenothiazine moiety, which is a linear tricyclic system that consists of a two benzene rings joined by a para-thiazine ring.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiazines
Sub ClassPhenothiazines
Direct ParentPhenothiazines
Alternative Parents
Substituents
  • Phenothiazine
  • Alkyldiarylamine
  • Diarylthioether
  • Benzenesulfonamide
  • N-alkylpiperazine
  • N-methylpiperazine
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Para-thiazine
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organonitrogen compound
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
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. Oades RD, Rao ML, Bender S, Sartory G, Muller BW: Neuropsychological and conditioned blocking performance in patients with schizophrenia: assessment of the contribution of neuroleptic dose, serum levels and dopamine D2-receptor occupancy. Behav Pharmacol. 2000 Jun;11(3-4):317-30. [PubMed:11103886 ]
  2. Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. [PubMed:11873706 ]
  3. Wu S, Xing Q, Gao R, Li X, Gu N, Feng G, He L: Response to chlorpromazine treatment may be associated with polymorphisms of the DRD2 gene in Chinese schizophrenic patients. Neurosci Lett. 2005 Mar 7;376(1):1-4. Epub 2004 Dec 2. [PubMed:15694263 ]
  4. Wu SN, Gao R, Xing QH, Li HF, Shen YF, Gu NF, Feng GY, He L: Association of DRD2 polymorphisms and chlorpromazine-induced extrapyramidal syndrome in Chinese schizophrenic patients. Acta Pharmacol Sin. 2006 Aug;27(8):966-70. [PubMed:16867246 ]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  6. Seeman P: Dopamine D2 receptors as treatment targets in schizophrenia. Clin Schizophr Relat Psychoses. 2010 Apr;4(1):56-73. doi: 10.3371/CSRP.4.1.5. [PubMed:20643630 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
antagonist
General Function:
G-protein coupled amine receptor activity
Specific Function:
Dopamine receptor whose activity is mediated by G proteins which activate adenylyl cyclase.
Gene Name:
DRD1
Uniprot ID:
P21728
Molecular Weight:
49292.765 Da
References
  1. Kanba S, Suzuki E, Nomura S, Nakaki T, Yagi G, Asai M, Richelson E: Affinity of neuroleptics for D1 receptor of human brain striatum. J Psychiatry Neurosci. 1994 Jul;19(4):265-9. [PubMed:7918347 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. Kusumi I, Takahashi Y, Suzuki K, Kameda K, Koyama T: Differential effects of subchronic treatments with atypical antipsychotic drugs on dopamine D2 and serotonin 5-HT2A receptors in the rat brain. J Neural Transm (Vienna). 2000;107(3):295-302. [PubMed:10821438 ]
  2. Yamada J, Sugimoto Y, Horisaka K: Serotonin2 (5-HT2) receptor agonist 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI) inhibits chlorpromazine- and haloperidol-induced hypothermia in mice. Biol Pharm Bull. 1995 Nov;18(11):1580-3. [PubMed:8593484 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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. 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. Cosi C, Koek W: Agonist, antagonist, and inverse agonist properties of antipsychotics at human recombinant 5-HT(1A) receptors expressed in HeLa cells. Eur J Pharmacol. 2001 Dec 14;433(1):55-62. [PubMed:11755134 ]
  2. Newman-Tancredi A, Gavaudan S, Conte C, Chaput C, Touzard M, Verriele L, Audinot V, Millan MJ: Agonist and antagonist actions of antipsychotic agents at 5-HT1A receptors: a [35S]GTPgammaS binding study. Eur J Pharmacol. 1998 Aug 21;355(2-3):245-56. [PubMed:9760039 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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.
Gene Name:
ADRA1A
Uniprot ID:
P35348
Molecular Weight:
51486.005 Da
References
  1. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. [PubMed:15695070 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
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.
Gene Name:
ADRA1B
Uniprot ID:
P35368
Molecular Weight:
56835.375 Da
References
  1. Cahir M, King DJ: Antipsychotics lack alpha 1A/B adrenoceptor subtype selectivity in the rat. Eur Neuropsychopharmacol. 2005 Mar;15(2):231-4. [PubMed:15695070 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. Kitamura K, Omran AA, Nagata C, Kamijima Y, Tanaka R, Takegami S, Kitade T: Effects of inorganic ions on the binding of triflupromazine and chlorpromazine to bovine serum albumin studied by spectrometric methods. Chem Pharm Bull (Tokyo). 2006 Jul;54(7):972-6. [PubMed:16819214 ]
  2. Rukhadze MD, Bezarashvili GS, Sidamonidze NS, Tsagareli SK: Investigation of binding process of chlorpromazine to bovine serum albumin by means of passive and active experiments. Biomed Chromatogr. 2001 Oct;15(6):365-73. [PubMed:11559920 ]
  3. Silva D, Cortez CM, Louro SR: Quenching of the intrinsic fluorescence of bovine serum albumin by chlorpromazine and hemin. Braz J Med Biol Res. 2004 Jul;37(7):963-8. Epub 2004 Jun 22. [PubMed:15264002 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Bednarczyk D, Ekins S, Wikel JH, Wright SH: Influence of molecular structure on substrate binding to the human organic cation transporter, hOCT1. Mol Pharmacol. 2003 Mar;63(3):489-98. [PubMed:12606755 ]
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Drug created on August 29, 2007 14:17 / Updated on August 17, 2016 12:23