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Identification
NameAcepromazine
Accession NumberDB01614
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

Acepromazine is one of the phenothiazine derivative psychotropic drugs, used little in humans, however frequently in animals as a sedative and antiemetic.

Structure
Thumb
Synonyms
1-[10-(3-DIMETHYLAMINO-propyl)-10H-phenothiazin-2-yl]-ethanone
10-(3-dimethylaminopropyl)phenothiazin-3-yl methyl ketone
10-(3-dimethylaminopropyl)phenothiazine-3-ethylone
Acetazine
Acetopromazine
Acetylpromazine
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
Acezine 2Not Available
AtravetNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Acepromazine maleate
ThumbNot applicableDBSALT001612
Categories
UNII54EJ303F0R
CAS number61-00-7
WeightAverage: 326.456
Monoisotopic: 326.145284026
Chemical FormulaC19H22N2OS
InChI KeyInChIKey=NOSIYYJFMPDDSA-UHFFFAOYSA-N
InChI
InChI=1S/C19H22N2OS/c1-14(22)15-9-10-19-17(13-15)21(12-6-11-20(2)3)16-7-4-5-8-18(16)23-19/h4-5,7-10,13H,6,11-12H2,1-3H3
IUPAC Name
1-{10-[3-(dimethylamino)propyl]-10H-phenothiazin-2-yl}ethan-1-one
SMILES
CN(C)CCCN1C2=CC=CC=C2SC2=C1C=C(C=C2)C(C)=O
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
  • Acetophenone
  • Aryl alkyl ketone
  • Aryl ketone
  • Benzoyl
  • Benzenoid
  • Para-thiazine
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ketone
  • Azacycle
  • Thioether
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationAcepromazine was first used in humans in the 1950s as an antipsychotic agent. It is now rarely used in humans. Acepromazine is frequently used in animals as a sedative and antiemetic. Its principal value is in quietening and calming anxious animals.
PharmacodynamicsAcepromazine is one of the phenothiazine derivative psychotropic drugs. Acepromazine has actions at all levels of the central nervous system-primarily at subcortical levels-as well as on multiple organ systems. Acepromazine has strong antiadrenergic and weaker peripheral anticholinergic activity; ganglionic blocking action is relatively slight. It also possesses slight antihistaminic and antiserotonin activity.
Mechanism of actionAcepromazine 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).
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half life3 hours in horses.
ClearanceNot Available
ToxicityAgitation, coma, convulsions, difficulty breathing, difficulty swallowing, dry mouth, extreme sleepiness, fever, intestinal blockage, irregular heart rate, low blood pressure, restlessness
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+0.9852
Blood Brain Barrier+0.9844
Caco-2 permeable+0.8203
P-glycoprotein substrateSubstrate0.8092
P-glycoprotein inhibitor IInhibitor0.8563
P-glycoprotein inhibitor IIInhibitor0.857
Renal organic cation transporterInhibitor0.7087
CYP450 2C9 substrateNon-substrate0.7438
CYP450 2D6 substrateSubstrate0.8618
CYP450 3A4 substrateSubstrate0.6468
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.9319
CYP450 2D6 inhibitorInhibitor0.9115
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9105
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7333
Ames testNon AMES toxic0.849
CarcinogenicityNon-carcinogens0.9292
BiodegradationNot ready biodegradable0.9829
Rat acute toxicity2.7963 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9537
hERG inhibition (predictor II)Inhibitor0.7813
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
StateLiquid
Experimental Properties
PropertyValueSource
melting point< 25 °CPhysProp
boiling point230 °C at 5.00E-01 mm HgPhysProp
Predicted Properties
PropertyValueSource
Water Solubility0.0098 mg/mLALOGPS
logP4.32ALOGPS
logP3.49ChemAxon
logS-4.5ALOGPS
pKa (Strongest Acidic)16.06ChemAxon
pKa (Strongest Basic)8.5ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area23.55 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity99.35 m3·mol-1ChemAxon
Polarizability37.17 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (7.84 KB)
SpectraNot Available
References
Synthesis ReferenceNot Available
General ReferencesNot Available
External Links
ATC CodesN05AA04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug Interactions
Drug
AcebutololAcepromazine may increase the hypotensive activities of Acebutolol.
Acetylsalicylic acidAcepromazine may increase the hypotensive activities of Acetylsalicylic acid.
AlfentanilAcepromazine may increase the hypotensive activities of Alfentanil.
AlmotriptanThe risk or severity of adverse effects can be increased when Almotriptan is combined with Acepromazine.
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Acepromazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Acepromazine.
AmoxapineThe risk or severity of adverse effects can be increased when Amoxapine is combined with Acepromazine.
AmphetamineAcepromazine may decrease the stimulatory activities of Amphetamine.
ArtemetherThe serum concentration of Acepromazine can be increased when it is combined with Artemether.
ArtesunateThe serum concentration of Acepromazine can be increased when it is combined with Artesunate.
AtovaquoneThe serum concentration of Acepromazine can be increased when it is combined with Atovaquone.
BenzphetamineAcepromazine may decrease the stimulatory activities of Benzphetamine.
BetaxololAcepromazine may increase the hypotensive activities of Betaxolol.
BisoprololAcepromazine may increase the hypotensive activities of Bisoprolol.
BuspironeThe risk or severity of adverse effects can be increased when Buspirone is combined with Acepromazine.
ButorphanolAcepromazine may increase the hypotensive activities of Butorphanol.
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Acepromazine.
CaffeineAcepromazine may increase the hypotensive activities of Caffeine.
Calcium carbonateCalcium carbonate can cause a decrease in the absorption of Acepromazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
CarteololAcepromazine may increase the hypotensive activities of Carteolol.
CarvedilolAcepromazine may increase the hypotensive activities of Carvedilol.
ChloroquineThe serum concentration of Acepromazine can be increased when it is combined with Chloroquine.
ChlorphenamineAcepromazine may increase the hypotensive activities of Chlorphenamine.
CitalopramThe risk or severity of adverse effects can be increased when Citalopram is combined with Acepromazine.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Acepromazine.
CodeineAcepromazine may increase the hypotensive activities of Codeine.
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Acepromazine.
DesipramineThe risk or severity of adverse effects can be increased when Desipramine is combined with Acepromazine.
DesvenlafaxineThe risk or severity of adverse effects can be increased when Desvenlafaxine is combined with Acepromazine.
DextroamphetamineAcepromazine may decrease the stimulatory activities of Dextroamphetamine.
DextromethorphanThe risk or severity of adverse effects can be increased when Dextromethorphan is combined with Acepromazine.
DihydrocodeineAcepromazine may increase the hypotensive activities of Dihydrocodeine.
DihydroergotamineThe risk or severity of adverse effects can be increased when Dihydroergotamine is combined with Acepromazine.
DonepezilDonepezil may increase the central neurotoxic activities of Acepromazine.
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Acepromazine.
DuloxetineThe risk or severity of adverse effects can be increased when Duloxetine is combined with Acepromazine.
EletriptanThe risk or severity of adverse effects can be increased when Eletriptan is combined with Acepromazine.
Ergoloid mesylateThe risk or severity of adverse effects can be increased when Ergoloid mesylate is combined with Acepromazine.
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Acepromazine.
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Acepromazine.
EscitalopramThe risk or severity of adverse effects can be increased when Escitalopram is combined with Acepromazine.
EsmololAcepromazine may increase the hypotensive activities of Esmolol.
FentanylAcepromazine may increase the hypotensive activities of Fentanyl.
FluoxetineThe risk or severity of adverse effects can be increased when Fluoxetine is combined with Acepromazine.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Acepromazine.
FrovatriptanThe risk or severity of adverse effects can be increased when Frovatriptan is combined with Acepromazine.
GalantamineGalantamine may increase the central neurotoxic activities of Acepromazine.
HydromorphoneAcepromazine may increase the hypotensive activities of Hydromorphone.
HydroxychloroquineThe serum concentration of Acepromazine can be increased when it is combined with Hydroxychloroquine.
ImipramineThe risk or severity of adverse effects can be increased when Imipramine is combined with Acepromazine.
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Acepromazine.
LabetalolAcepromazine may increase the hypotensive activities of Labetalol.
LevomilnacipranThe risk or severity of adverse effects can be increased when Levomilnacipran is combined with Acepromazine.
LevorphanolAcepromazine may increase the hypotensive activities of Levorphanol.
LinezolidThe risk or severity of adverse effects can be increased when Linezolid is combined with Acepromazine.
LisdexamfetamineAcepromazine may decrease the stimulatory activities of Lisdexamfetamine.
LithiumLithium may increase the neurotoxic activities of Acepromazine.
LorcaserinThe risk or severity of adverse effects can be increased when Lorcaserin is combined with Acepromazine.
LumefantrineThe serum concentration of Acepromazine can be increased when it is combined with Lumefantrine.
Magnesium hydroxideMagnesium hydroxide can cause a decrease in the absorption of Acepromazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
MaprotilineThe risk or severity of adverse effects can be increased when Maprotiline is combined with Acepromazine.
MefloquineThe serum concentration of Acepromazine can be increased when it is combined with Mefloquine.
MethadoneAcepromazine may increase the hypotensive activities of Methadone.
MethamphetamineAcepromazine may decrease the stimulatory activities of Methamphetamine.
MethylphenidateThe risk or severity of adverse effects can be increased when Acepromazine is combined with Methylphenidate.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Acepromazine.
MetoprololAcepromazine may increase the hypotensive activities of Metoprolol.
MetyrosineThe risk or severity of adverse effects can be increased when Metyrosine is combined with Acepromazine.
MilnacipranThe risk or severity of adverse effects can be increased when Milnacipran is combined with Acepromazine.
MoclobemideThe risk or severity of adverse effects can be increased when Moclobemide is combined with Acepromazine.
MorphineAcepromazine may increase the hypotensive activities of Morphine.
NalbuphineAcepromazine may increase the hypotensive activities of Nalbuphine.
NaratriptanThe risk or severity of adverse effects can be increased when Naratriptan is combined with Acepromazine.
NebivololAcepromazine may increase the hypotensive activities of Nebivolol.
NefazodoneThe risk or severity of adverse effects can be increased when Acepromazine is combined with Nefazodone.
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Acepromazine.
OxycodoneAcepromazine may increase the hypotensive activities of Oxycodone.
OxymorphoneAcepromazine may increase the hypotensive activities of Oxymorphone.
ParoxetineThe risk or severity of adverse effects can be increased when Paroxetine is combined with Acepromazine.
PenbutololAcepromazine may increase the hypotensive activities of Penbutolol.
PentazocineAcepromazine may increase the hypotensive activities of Pentazocine.
PethidineAcepromazine may increase the hypotensive activities of Pethidine.
PhendimetrazineAcepromazine may decrease the stimulatory activities of Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Acepromazine.
PhentermineAcepromazine may decrease the stimulatory activities of Phentermine.
PindololAcepromazine may increase the hypotensive activities of Pindolol.
PrimaquineThe serum concentration of Acepromazine can be increased when it is combined with Primaquine.
ProcarbazineThe risk or severity of adverse effects can be increased when Procarbazine is combined with Acepromazine.
ProguanilThe serum concentration of Acepromazine can be increased when it is combined with Proguanil.
PromethazineThe risk or severity of adverse effects can be increased when Promethazine is combined with Acepromazine.
PropranololAcepromazine may increase the hypotensive activities of Propranolol.
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Acepromazine.
PyrimethamineThe serum concentration of Acepromazine can be increased when it is combined with Pyrimethamine.
QuinagolideThe therapeutic efficacy of Quinagolide can be decreased when used in combination with Acepromazine.
QuinineThe serum concentration of Acepromazine can be increased when it is combined with Quinine.
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Acepromazine.
RemifentanilAcepromazine may increase the hypotensive activities of Remifentanil.
RivastigmineRivastigmine may increase the central neurotoxic activities of Acepromazine.
RizatriptanThe risk or severity of adverse effects can be increased when Rizatriptan is combined with Acepromazine.
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Acepromazine.
SertralineThe risk or severity of adverse effects can be increased when Sertraline is combined with Acepromazine.
Sodium bicarbonateSodium bicarbonate can cause a decrease in the absorption of Acepromazine resulting in a reduced serum concentration and potentially a decrease in efficacy.
SotalolAcepromazine may increase the hypotensive activities of Sotalol.
SufentanilAcepromazine may increase the hypotensive activities of Sufentanil.
SumatriptanThe risk or severity of adverse effects can be increased when Sumatriptan is combined with Acepromazine.
Tedizolid PhosphateThe risk or severity of adverse effects can be increased when Tedizolid Phosphate is combined with Acepromazine.
TetrabenazineThe risk or severity of adverse effects can be increased when Tetrabenazine is combined with Acepromazine.
TimololAcepromazine may increase the hypotensive activities of Timolol.
TramadolAcepromazine may increase the hypotensive activities of Tramadol.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Acepromazine.
TrazodoneThe risk or severity of adverse effects can be increased when Acepromazine is combined with Trazodone.
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Acepromazine.
VenlafaxineThe risk or severity of adverse effects can be increased when Venlafaxine is combined with Acepromazine.
VilazodoneThe risk or severity of adverse effects can be increased when Vilazodone is combined with Acepromazine.
VortioxetineThe risk or severity of adverse effects can be increased when Vortioxetine is combined with Acepromazine.
ZolmitriptanThe risk or severity of adverse effects can be increased when Zolmitriptan is combined with Acepromazine.
Food Interactions
  • Avoid alcohol
  • Take with food to reduce irritation

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
yes
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
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.
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
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.
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 ]
Comments
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Drug created on August 29, 2007 14:12 / Updated on February 04, 2016 11:34