Title : Characterization of human cytochrome P450 enzymes involved in the in vitro metabolism of perospirone.

Pub. Date : 2005 Mar

PMID : 15619261






2 Functional Relationships(s)
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1 In vitro studies were carried out to identify the major contribution of CYP2C8, CYP2D6 and CYP3A4 to the metabolism of perospirone (cis-N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]cyclohexane-1,2-dicarboximide monohydrochloride dehydrate), a novel antipsychotic agent, using human liver microsomes and expressed P450 isoforms. perospirone cytochrome P450 family 3 subfamily A member 4 Homo sapiens
2 These results indicated that the metabolism of perospirone in human liver was mainly catalysed by CYP3A4, and to a lesser extent CYP2C8 and CYP2D6 were responsible because kinetic data (K(m) and V(max)) of CYP2C8 and CYP2D6 suggested catalytic potential. perospirone cytochrome P450 family 3 subfamily A member 4 Homo sapiens