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Cerebral pharmacokinetics of ipsapirone in rats after different routes of administration

Nocon, H.; Daniel, W.; Danek, L.; Melzacka, M.

Journal of Pharmacy and Pharmacology 42(9): 642-645

1990

ISSN/ISBN: 0022-3573
PMID: 1981903
Document Number: 359832
Ipsapirone, a putative non-benzodiazepine anxiolytic, was extensively metabolized in rats to 1-(2-pyrimidinyl)piperazine (1-PP) which accumulated in the brain. Neither the route of administration (i.p. or p.o.), nor prolonged administration of ipsapirone or 1-PP affected their accumulation in the rat brain. The cytochrome P450 level and ethylmorphine N-demethylase activity in rat liver microsomes were unchanged by chronic treatment with ipsapirone or 1-PP. The results indicate that 1-PP may contribute to the .alpha.2-adrenoceptor antagonism of ipsapirone in rats and that chronic treatment with the drug does not affect its biotransformation to 1-PP.

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