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Drug-Target Interaction

Drug

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PubChem ID:4744
Structure:
Synonyms:
10-(3-(4-Methyl-1-piperazinyl)propyl)-10H-phenothiazine
10-(g-methylpiperazinopropyl)phenothiazine
10-[3-(4-methylpiperazin-1-yl)propyl]-10H-phenothiazine
10-[3-(4-methylpiperazin-1-yl)propyl]phenothiazine
10H-Phenothiazine, 10-(3-(4-methyl-1-piperazinyl)propyl)-
10H-Phenothiazine, 10-[3-(4-methyl-1-piperazinyl)propyl]-
14516-56-4
14516-56-4 (maleate (1:2))
5317-37-3
5317-37-3 (di-hydrochloride)
6002-77-3
6002-77-3 (maleate)
84-97-9
AC1L1IUZ
AC1Q7G55
AIDS-136667
AIDS136667
AKOS000281842
AR-1B9998
C16903
C20H25N3S
CHEBI:59118
CHEMBL1697766
EINECS 201-578-9
LS-105589
N-(3-(4-Methyl-1-piperazinyl)propyl)phenothiazine
N-Methyl-piperazinyl-N'-propyl-phenothiazin
N-Methyl-piperazinyl-N'-propyl-phenothiazin [German]
N-Methyl-piperazinylpropyl-phenothiazine
NCGC00159492-02
NCGC00159492-03
NSC638694
P 725
PERAZINE
Perazine Fendizoate (perazine)
Pernazine
Phenothiazine, 10-(3-(4-methyl-1-piperazinyl)propyl)-
Psytomin
Taxilan
UNII-8915147A2B
ATC-Codes:

Target

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Uniprot ID:CP1A2_HUMAN
Synonyms:
CYPIA2
Cytochrome P450 1A2
P(3)450
P450 4
P450-P3
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:2HI4
Structure:
2HI4

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----
----
----
----

References:

12523495
Perazine as a potent inhibitor of human CYP1A2 but not CYP3A4.. Jacek Wójcikowski; Lydiane Pichard-Garcia; Patrick Maurel; W?adys?awa A Daniel (2002) Polish journal of pharmacology display abstract
The effects of perazine on the activities of CYP1A2 and CYP3A4 in a primary culture of human hepatocytes of one patient were studied in vitro. The CYPs activities were assessed by measuring the rate of acetanilide 4-hydroxylation (CYP1A2) and cyclosporine A oxidation (CYP3A4) after treatment with TCDD (a CYP1A subfamily inducer) or rifampicin (mainly a CYP3A4 inducer). The amounts of the metabolites formed in hepatocytes were assayed in the extracellular medium using the HPLC method. TCDD and rifampicin induced the formation of 4-hydroxyacetanilide and cyclosporine A metabolites (monohydroxycyclosporine A, dihydroxycyclosporine A, N-desmethylcyclosporine A), respectively. The formation of 4-hydroxyacetanilide was strongly inhibited by three different concentrations of perazine (10, 25 and 50 microM) reaching 8, 3 and 2% of the control value, respectively. In the case of CYP3A4 activity, no such an effect of perazine was observed. Perazine showed only a week inhibition of the activity of cyclosporine A oxidase (to 96-86% of the control value). The obtained results suggest a strong inhibitory effect of perazine on human CYP1A2 activity with predicted Ki value similar to those of the known for CYP1A2 inhibitors, such as furafylline and fluvoxamine.
12523495
Perazine as a potent inhibitor of human CYP1A2 but not CYP3A4.. Jacek Wójcikowski; Lydiane Pichard-Garcia; Patrick Maurel; W?adys?awa A Daniel (2002) Polish journal of pharmacology display abstract
The effects of perazine on the activities of CYP1A2 and CYP3A4 in a primary culture of human hepatocytes of one patient were studied in vitro. The CYPs activities were assessed by measuring the rate of acetanilide 4-hydroxylation (CYP1A2) and cyclosporine A oxidation (CYP3A4) after treatment with TCDD (a CYP1A subfamily inducer) or rifampicin (mainly a CYP3A4 inducer). The amounts of the metabolites formed in hepatocytes were assayed in the extracellular medium using the HPLC method. TCDD and rifampicin induced the formation of 4-hydroxyacetanilide and cyclosporine A metabolites (monohydroxycyclosporine A, dihydroxycyclosporine A, N-desmethylcyclosporine A), respectively. The formation of 4-hydroxyacetanilide was strongly inhibited by three different concentrations of perazine (10, 25 and 50 microM) reaching 8, 3 and 2% of the control value, respectively. In the case of CYP3A4 activity, no such an effect of perazine was observed. Perazine showed only a week inhibition of the activity of cyclosporine A oxidase (to 96-86% of the control value). The obtained results suggest a strong inhibitory effect of perazine on human CYP1A2 activity with predicted Ki value similar to those of the known for CYP1A2 inhibitors, such as furafylline and fluvoxamine.
14581727
14581727
15056479