CEREBRAL PHARMACOKINETICS OF IPSAPIRONE IN RATS AFTER DIFFERENT ROUTES OF ADMINISTRATION

被引：18

作者：

NOCON, H ^{[1
]}

DANIEL, W ^{[1
]}

DANEK, L ^{[1
]}

MELZACKA, M ^{[1
]}

机构：

[1] POLISH ACAD SCI,INST PHARMACOL,PL-31343 KRAKOW,POLAND

来源：

JOURNAL OF PHARMACY AND PHARMACOLOGY | 1990年 / 42卷 / 09期

关键词：

D O I：

10.1111/j.2042-7158.1990.tb06623.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Abstract— 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 α2‐adrenoceptor antagonism of ipsapirone in rats and that chronic treatment with the drug does not affect its biotransformation to 1‐PP. 1990 Royal Pharmaceutical Society of Great Britain

引用

页码：642 / 645

页数：4

共 13 条

[1] THE ALPHA2-ADRENOCEPTOR ANTAGONIST ACTIVITY OF IPSAPIRONE AND GEPIRONE IS MEDIATED BY THEIR COMMON METABOLITE 1-(2-PYRIMIDINYL)-PIPERAZINE (PMP) [J].