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Drug-Target Interaction

Drug

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PubChem ID:3025899
Structure:
Synonyms:
164352-89-0
2-(Allylthio)pyrazine
2-prop-2-enylsulfanylpyrazine
AC1MHG6G
C104935
CID3025899
LS-127561

Target

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Uniprot ID:CP2B1_RAT
Synonyms:
CYPIIB1
Cytochrome P450 2B1
P450-B
P450-LM2
P450-PB1 and P450-PB2
P450b
EC-Numbers:1.14.14.1
Organism:Rat
Rattus norvegicus
PDB IDs:-

Binding Affinities:

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

References:

9920347
2-(allylthio)pyrazine inhibition of aflatoxin B1-induced hepatotoxicity in rats: inhibition of cytochrome P450 2B- and 3A2-mediated bioactivation.. T G Ha; N D Kim (1998) Research communications in molecular pathology and pharmacology display abstract
2-(Allylthio)pyrazine (2-AP), a synthetic organosulfur compound, exhibits hepatoprotective and chemopreventive effects. The effects of 2-AP on aflatoxin B1 (AFB1)-induced hepatotoxicity was studied in rats. 2-AP treatment substantially reduced AFB1-induced toxicity, as evidenced by reduction in the mortality rate of animals as well as decreases in serum alanine aminotransferase and sorbitol dehydrogenase activities. AFB -induced lipid peroxidation was also significantly reduced in rats by 2-AP treatment. Studies were extended to determine whether 2-AP was active in inhibiting cytochrome P450-mediated metabolic activation of AFB1. Covalent binding of AFB1 to calf thymus DNA in the presence of S-9 fraction was inhibited by 2-AP in vitro. Hepatic microsomal pentoxyresorufin-O-depentylase and ethoxyresorufin-O-deethylase activities were also potently inhibited by 2-AP. These results demonstrated that 2-AP was effective in protecting the liver against AFB1-induced toxicity and the mechanism of chemoprotection by 2-AP might involve inhibition of the P450 2B- and 3A2-mediated metabolism of AFB1.