DT-Web

DB01608 - Propericiazine


Identification
Name Propericiazine
Accession Number DB01608
Type small molecule
Description Propericiazine is a phenothiazine of the piperidine group. It has been shown to reduce pathologic arousal and affective tension in some psychotic patients, while the symptoms of abnormal mental integration are relatively unaffected. It is a sedative phenothiazine with weak antipsychotic properties. It also has adrenolytic, anticholinergic, metabolic and endocrine effects and an action on the extrapyramidal system. It is used as an adjunctive medication in some psychotic patients, for the control of residual prevailing hostility, impulsiveness and aggressiveness. Pericyazine, like other phenothiazines, is presumed to act principally in the subcortical areas, by producing what has been described as a central adrenergic blockade.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 365.492
Groups approved
Monoisotopic Weight 365.156183063
Pharmacology
Indication For use as adjunctive medication in some psychotic patients. Propericiazine (Pericyazine)is used for the control of residual prevailing hostility, impulsiveness and aggressiveness.
Mechanism of action Pericyazine, like other phenothiazines, is presumed to act principally in the subcortical areas, by producing what has been described as a central adrenergic blockade of the alpha adrenergic receptors as well as antagonism of the D(1) dopamine receptor.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity In milder cases of phenothiazine overdosage the patient may be agitated, delirious and confused. Frequently he is lethargic or in a comatose state. Twitching, dystonic movements or convulsions may be present and hypotension, cardiovascular collapse, arrhythmias and hypothermia might be observed.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Amphetamine Decreased anorexic effect, may increase pyschotic symptoms
Benzphetamine Antipsychotics may diminish the stimulatory effect of Amphetamines. Monitor effectiveness of amphetamine therapy when altering concurrent antipsychotic therapy as antipsychotic agents may impair the stimulatory effect of amphetamines.
Dexfenfluramine Decreased anorexic effect, may increase psychotic symptoms.
Dextroamphetamine Decreased anorexic effect, may increase pyschotic symptoms
Diethylpropion Decreased anorexic effect, may increase psychotic symptoms.
Donepezil Possible antagonism of action
Fenfluramine Decreased anorexic effect, may increase psychotic symptoms.
Galantamine Possible antagonism of action
Guanethidine Propericiazine may decrease the effect of guanethidine.
Mazindol Decreased anorexic effect, may increase psychotic symptoms.
Methamphetamine Decreased anorexic effect, may increase pyschotic symptoms
Metrizamide Increased risk of convulsions
Phendimetrazine Decreased anorexic effect, may increase pyschotic symptoms
Phenmetrazine Decreased anorexic effect, may increase pyschotic symptoms
Phentermine Decreased anorexic effect, may increase psychotic symptoms.
Phenylpropanolamine Decreased anorexic effect, may increase psychotic symptoms.
Rivastigmine Possible antagonism of action
Terfenadine Increased risk of cardiotoxicity and arrhythmias
Food Interactions
  • Take with food to reduce irritation. Avoid alcohol.

Targets


D(1A) dopamine receptor
Name D(1A) dopamine receptor
Gene Name DRD1
Pharmacological action yes
Actions antagonist
References
  • 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
DTHybrid score 0.2491
Alpha-2A adrenergic receptor
Name Alpha-2A adrenergic receptor
Gene Name ADRA2A
Pharmacological action yes
Actions antagonist
References
  • Tsukamoto T, Asakura M, Hirata N, Imafuku J, Matsui H, Hasegawa K: Interaction of neuroleptics and antidepressants with rat brain alpha 2-receptors: a possible relationship between alpha 2-receptor antagonism and antidepressant action. Biol Psychiatry. 1984 Sep;19(9):1283-91. - Pubmed
DTHybrid score 0.3162
Alpha-1B adrenergic receptor
Name Alpha-1B adrenergic receptor
Gene Name ADRA1B
Pharmacological action unknown
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
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.247

Predictions


Id Partner name Gene Name Score
556 Alpha-1A adrenergic receptor ADRA1A 0.2439
831 D(2) dopamine receptor DRD2 0.1531
502 5-hydroxytryptamine 2A receptor HTR2A 0.1255
629 Alpha-2B adrenergic receptor ADRA2B 0.1167
378 Alpha-2C adrenergic receptor ADRA2C 0.1098
789 Alpha-1D adrenergic receptor ADRA1D 0.0982
4119 Cytochrome P450 2D6 CYP2D6 0.0887
320 5-hydroxytryptamine 1A receptor HTR1A 0.0825
590 5-hydroxytryptamine 2C receptor HTR2C 0.0804
4512 Cytochrome P450 3A4 CYP3A4 0.0801
163 D(1B) dopamine receptor DRD5 0.0773
432 D(4) dopamine receptor DRD4 0.0768
4200 Cytochrome P450 1A2 CYP1A2 0.0691
638 D(3) dopamine receptor DRD3 0.0635
725 5-hydroxytryptamine 1D receptor HTR1D 0.0547
492 Histamine H1 receptor HRH1 0.0504
885 5-hydroxytryptamine 1B receptor HTR1B 0.047
1588 Multidrug resistance protein 1 ABCB1 0.0444
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0428
436 5-hydroxytryptamine 2B receptor HTR2B 0.0428
713 Sodium-dependent dopamine transporter SLC6A3 0.0413
103 Muscarinic acetylcholine receptor M1 CHRM1 0.0354
6145 Solute carrier family 22 member 1 SLC22A1 0.0331
716 5-hydroxytryptamine 7 receptor HTR7 0.0321
193 Beta-1 adrenergic receptor ADRB1 0.031
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0282
766 Beta-2 adrenergic receptor ADRB2 0.028
6016 Cytochrome P450 2C19 CYP2C19 0.0274
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0274
824 Sodium-dependent serotonin transporter SLC6A4 0.0273
617 Muscarinic acetylcholine receptor M2 CHRM2 0.0271
3941 Amine oxidase [flavin-containing] A MAOA 0.0259
4757 Cytochrome P450 2C9 CYP2C9 0.0246
51 Muscarinic acetylcholine receptor M3 CHRM3 0.0244
1256 5-hydroxytryptamine 6 receptor HTR6 0.0236
4118 Cytochrome P450 3A5 CYP3A5 0.0218
587 Serum albumin ALB 0.0209
101 Potassium voltage-gated channel subfamily H member 2 KCNH2 0.0198
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0195
6013 Cytochrome P450 2E1 CYP2E1 0.0184
131 Synaptic vesicular amine transporter SLC18A2 0.0168
528 5-hydroxytryptamine 1E receptor HTR1E 0.0163
341 5-hydroxytryptamine 3 receptor HTR3A 0.015
6107 Cytochrome P450 3A7 CYP3A7 0.0145
1539 Oligopeptide transporter, small intestine isoform SLC15A1 0.0145
828 Phenylalanine-4-hydroxylase PAH 0.0132
3109 Phenylalanine-4-hydroxylase phhA 0.0132
6144 Solute carrier family 22 member 2 SLC22A2 0.013
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0129
514 Potassium voltage-gated channel subfamily H member 6 KCNH6 0.0128
772 Potassium voltage-gated channel subfamily H member 7 KCNH7 0.0128
6147 Solute carrier family 22 member 3 SLC22A3 0.0119
1517 Beta-3 adrenergic receptor ADRB3 0.0114
6030 Cytochrome P450 2B6 CYP2B6 0.0113
3923 Cholinesterase BCHE 0.0107
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0105
3426 Glutamine synthetase glnA 0.0103
3987 Glutamine synthetase GLUL 0.0103
465 Calmodulin CALM1 0.0101
3810 Catechol O-methyltransferase COMT 0.0099
118 Organic cation/carnitine transporter 2 SLC22A5 0.0098
6024 Cytochrome P450 1A1 CYP1A1 0.0093
1636 Trace amine-associated receptor 1 TAAR1 0.009
4924 Cytochrome P450 2C8 CYP2C8 0.0087
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0084
6164 POU domain, class 5, transcription factor 1 POU5F1 0.0078
6070 Nischarin NISCH 0.0075
3939 Amine oxidase [flavin-containing] B MAOB 0.0075
124 Histamine H2 receptor HRH2 0.0072
6138 Multidrug resistance protein 3 ABCB4 0.007
709 ATP-sensitive inward rectifier potassium channel 1 KCNJ1 0.0068
6020 Aldehyde oxidase AOX1 0.0062
6151 Monocarboxylate transporter 10 SLC16A10 0.0058
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0053
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.005
1656 CYP2B protein CYP2B 0.0048
1632 Solute carrier organic anion transporter family member 2B1 SLCO2B1 0.0042
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.004
6178 UDP-glucuronosyltransferase 2B7 UGT2B7 0.004
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.004
233 Potassium channel subfamily K member 2 KCNK2 0.0039
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0039
4120 NADPH--cytochrome P450 reductase POR 0.0037
4114 Voltage-dependent L-type calcium channel subunit beta-3 CACNB3 0.0034
4112 Voltage-dependent L-type calcium channel subunit beta-4 CACNB4 0.0033
866 Large neutral amino acids transporter small subunit 2 SLC7A8 0.0033
164 Histamine H4 receptor HRH4 0.0033
776 Bile salt export pump ABCB11 0.0032
4113 Voltage-dependent L-type calcium channel subunit alpha-1F CACNA1F 0.0031
245 Large neutral amino acids transporter small subunit 1 SLC7A5 0.0031
333 Voltage-dependent L-type calcium channel subunit beta-1 CACNB1 0.003
158 Sodium channel protein type 1 subunit alpha SCN1A 0.0029
696 Kappa-type opioid receptor OPRK1 0.0026
4111 Voltage-dependent L-type calcium channel subunit alpha-1S CACNA1S 0.0026
6106 Cytochrome P450 2C18 CYP2C18 0.0024
474 Acetylcholinesterase ACHE 0.0023
464 Glutamate [NMDA] receptor subunit epsilon-2 GRIN2B 0.0022
5251 Carbonyl reductase [NADPH] 1 CBR1 0.0021
153 Dopamine beta-hydroxylase DBH 0.002
1898 Cytochrome P450 1B1 CYP1B1 0.0019
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0018
1732 ATP-binding cassette sub-family G member 2 ABCG2 0.0017
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0017
833 Organic cation/carnitine transporter 1 SLC22A4 0.0017
6018 UDP-glucuronosyltransferase 1-9 UGT1A9 0.0016
5718 Cytochrome P450 2A6 CYP2A6 0.0016
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0014
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0013
1618 High affinity nerve growth factor receptor NTRK1 0.001
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.001
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.001
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.001
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0008
467 Delta-type opioid receptor OPRD1 0.0007
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