DT-Web

DB01063 - Acetophenazine


Identification
Name Acetophenazine
Accession Number DB01063 (APRD00462)
Type small molecule
Description Acetophenazine is an antipsychotic drug of moderate-potency. It is used in the treatment of disorganized and psychotic thinking. It is also used to help treat false perceptions (e.g. hallucinations or delusions). It primarily targets the dopamine D2 receptor.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 411.56
Groups approved
Monoisotopic Weight 411.198047877
Pharmacology
Indication For the treatment of disorganized and psychotic thinking. Also used to help treat false perceptions (e.g. hallucinations or delusions.)
Mechanism of action Acetophenazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Not Available
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Bromocriptine The phenothiazine decreases the effect of bromocriptine
Cisapride Increased risk of cardiotoxicity and arrhythmias
Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms
Diethylpropion Decreased anorexic effect, may increase psychotic symptoms
Fenfluramine Decreased anorexic effect, may increase psychotic symptoms
Guanethidine Acetophenazine may decrease the effect of guanethidine.
Mazindol Decreased anorexic effect, may increase psychotic symptoms
Phentermine Decreased anorexic effect, may increase psychotic symptoms
Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Acetophenazine, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. Similar pharmacologic properties thus combination therapy will worsen the severity of sedative, parkinsonian, and extrapyramidal adverse effects.
Trimethobenzamide Trimethobenzamide and Acetophenazine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine The antihistamine, Triprolidine, may increase the arrhythmogenic effect of the phenothiazine, Acetophenazine. Monitor for symptoms of ventricular arrhythmias. Additive anticholinergic and CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
Trospium Trospium and Acetophenazine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Food Interactions Not Available

Targets


D(2) dopamine receptor
Name D(2) dopamine receptor
Gene Name DRD2
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Seeman P: Atypical antipsychotics: mechanism of action. Can J Psychiatry. 2002 Feb;47(1):27-38. - Pubmed
  • Tam SW, Cook L: Sigma opiates and certain antipsychotic drugs mutually inhibit (+)-[3H] SKF 10,047 and [3H]haloperidol binding in guinea pig brain membranes. Proc Natl Acad Sci U S A. 1984 Sep;81(17):5618-21. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.3158
D(1A) dopamine receptor
Name D(1A) dopamine receptor
Gene Name DRD1
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
DTHybrid score 0.2557

Predictions


Id Partner name Gene Name Score
502 5-hydroxytryptamine 2A receptor HTR2A 0.1354
638 D(3) dopamine receptor DRD3 0.0786
432 D(4) dopamine receptor DRD4 0.0782
556 Alpha-1A adrenergic receptor ADRA1A 0.0781
4119 Cytochrome P450 2D6 CYP2D6 0.0777
163 D(1B) dopamine receptor DRD5 0.0744
320 5-hydroxytryptamine 1A receptor HTR1A 0.0692
318 Alpha-2A adrenergic receptor ADRA2A 0.0668
590 5-hydroxytryptamine 2C receptor HTR2C 0.0632
632 Alpha-1B adrenergic receptor ADRA1B 0.0553
629 Alpha-2B adrenergic receptor ADRA2B 0.0511
4512 Cytochrome P450 3A4 CYP3A4 0.0502
378 Alpha-2C adrenergic receptor ADRA2C 0.0484
4200 Cytochrome P450 1A2 CYP1A2 0.0459
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0417
436 5-hydroxytryptamine 2B receptor HTR2B 0.04
725 5-hydroxytryptamine 1D receptor HTR1D 0.0358
1588 Multidrug resistance protein 1 ABCB1 0.0354
885 5-hydroxytryptamine 1B receptor HTR1B 0.0318
492 Histamine H1 receptor HRH1 0.0309
716 5-hydroxytryptamine 7 receptor HTR7 0.0288
6145 Solute carrier family 22 member 1 SLC22A1 0.0273
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0233
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0208
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0202
6016 Cytochrome P450 2C19 CYP2C19 0.0197
587 Serum albumin ALB 0.0196
789 Alpha-1D adrenergic receptor ADRA1D 0.0188
51 Muscarinic acetylcholine receptor M3 CHRM3 0.018
1256 5-hydroxytryptamine 6 receptor HTR6 0.0178
4757 Cytochrome P450 2C9 CYP2C9 0.0169
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0169
465 Calmodulin CALM1 0.0168
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0155
6013 Cytochrome P450 2E1 CYP2E1 0.0154
4118 Cytochrome P450 3A5 CYP3A5 0.015
6107 Cytochrome P450 3A7 CYP3A7 0.0139
3923 Cholinesterase BCHE 0.0135
824 Sodium-dependent serotonin transporter SLC6A4 0.0117
3941 Amine oxidase [flavin-containing] A MAOA 0.0111
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0102
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0101
528 5-hydroxytryptamine 1E receptor HTR1E 0.0098
4924 Cytochrome P450 2C8 CYP2C8 0.0091
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0088
750 Voltage-dependent calcium channel gamma-1 subunit CACNG1 0.0087
6030 Cytochrome P450 2B6 CYP2B6 0.0081
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0078
341 5-hydroxytryptamine 3 receptor HTR3A 0.0077
923 Glutamate receptor 3 GRIA3 0.0074
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0074
6144 Solute carrier family 22 member 2 SLC22A2 0.0066
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0063
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0062
131 Synaptic vesicular amine transporter SLC18A2 0.006
193 Beta-1 adrenergic receptor ADRB1 0.006
866 Large neutral amino acids transporter small subunit 2 SLC7A8 0.0057
3426 Glutamine synthetase glnA 0.0056
3987 Glutamine synthetase GLUL 0.0056
245 Large neutral amino acids transporter small subunit 1 SLC7A5 0.0053
713 Sodium-dependent dopamine transporter SLC6A3 0.0051
174 Sigma 1-type opioid receptor SIGMAR1 0.0048
3939 Amine oxidase [flavin-containing] B MAOB 0.0047
921 Glutamate receptor 2 GRIA2 0.0045
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0043
6106 Cytochrome P450 2C18 CYP2C18 0.0042
6024 Cytochrome P450 1A1 CYP1A1 0.0042
6859 Protein S100-A4 S100A4 0.0041
474 Acetylcholinesterase ACHE 0.0041
94 5-hydroxytryptamine 4 receptor HTR4 0.004
694 Matrix protein 2 M 0.0039
6151 Monocarboxylate transporter 10 SLC16A10 0.0038
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0038
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0036
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0036
380 Cytochrome P450 17A1 CYP17A1 0.0035
427 Substance-P receptor TACR1 0.0034
153 Dopamine beta-hydroxylase DBH 0.0034
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0032
124 Histamine H2 receptor HRH2 0.0032
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0031
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0029
3810 Catechol O-methyltransferase COMT 0.0027
1561 Troponin C, slow skeletal and cardiac muscles TNNC1 0.0027
776 Bile salt export pump ABCB11 0.0027
6147 Solute carrier family 22 member 3 SLC22A3 0.0024
118 Organic cation/carnitine transporter 2 SLC22A5 0.0021
5718 Cytochrome P450 2A6 CYP2A6 0.002
3947 Xanthine dehydrogenase/oxidase XDH 0.002
164 Histamine H4 receptor HRH4 0.002
766 Beta-2 adrenergic receptor ADRB2 0.0018
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0018
15 Voltage-dependent T-type calcium channel subunit alpha-1I CACNA1I 0.0018
20 Prostaglandin G/H synthase 1 PTGS1 0.0017
535 Voltage-dependent T-type calcium channel subunit alpha-1G CACNA1G 0.0017
964 Voltage-dependent T-type calcium channel subunit alpha-1H CACNA1H 0.0016
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0015
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0015
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0014
1898 Cytochrome P450 1B1 CYP1B1 0.0011
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