Cerebral pharmacokinetics of ipsapirone in rats after different routes of administration
| Autor: | Halina Nocon, Władysława A. Daniel, L Danek, M Melzacka |
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| Rok vydání: | 1990 |
| Předmět: |
Male
medicine.medical_specialty medicine.drug_class Metabolite Pharmaceutical Science Alpha (ethology) Administration Oral Biology Pharmacology Anxiolytic Route of administration chemistry.chemical_compound Pharmacokinetics Cytochrome P-450 Enzyme System Internal medicine medicine Animals Biotransformation Chromatography High Pressure Liquid Proadifen Ipsapirone Ethylmorphine-N-Demethylase Cytochrome P450 Brain Rats Inbred Strains Ethylmorphine Rats Endocrinology Pyrimidines chemistry Anti-Anxiety Agents biology.protein Microsomes Liver Injections Intraperitoneal medicine.drug Half-Life |
| Zdroj: | The Journal of pharmacy and pharmacology. 42(9) |
| ISSN: | 0022-3573 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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