Disposition of the psychotropic drugs buspirone, MJ-13805 and piribedil, and of their common active metabolite 1-(2-pyrimidinyl)-piperazine in the rat
1985; Taylor & Francis; Volume: 15; Issue: 10 Linguagem: Inglês
10.3109/00498258509045035
ISSN1366-5928
AutoresSilvio Caccia, M.H. Fong, Giovanna Guiso,
Tópico(s)Nicotinic Acetylcholine Receptors Study
Resumo1. 1-(2-Pyrimidinyl)-piperazine (PmP) is a common metabolite of the structurally related drugs buspirone, MJ-13805 and piribedil.2. After i.v. injection (25 μmol/kg) to rats, all three parent drugs are rapidly cleared with a t1/2 (β) of about 30 min. The metabolite t1/2 is about four times that of its parent drugs.3. About 25, 23 and 2% of buspirone, MJ-13805 and piribedil, respectively, reaches the systemic circulation as PmP. The metabolite concentrates in the brain where its A.U.C. is about twice those of buspirone and MJ-13805.4. Results indicate that PmP formation is a pharmacologically significant process for both buspirone and MJ-13805 but it is probably less important for piribedil.
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