Giral P, Soubrie P, Puech A J
Eur J Pharmacol. 1987 Jan 28;134(1):113-6. doi: 10.1016/0014-2999(87)90139-7.
We investigated in mice the effects of one of the principal metabolites of buspirone and gepirone, 1-(2-pyridinyl)-piperazine (1-PmP), on hypothermia and reduced locomotion induced by clonidine (0.25 and 0.06 mg/kg, respectively), tests related to brain alpha-adrenergic function. Both effects were antagonized dose dependently by 1-PmP (1-16 mg/kg i.p.). Moreover, pretreatment with proadifen (50 mg/kg) prevented the reversal by buspirone and gepirone of clonidine-induced hypothermia. This suggests that 1-PmP could be responsible for some of the apparent noradrenergic effects of buspirone and gepirone.
我们在小鼠中研究了丁螺环酮和吉哌隆的主要代谢产物之一1-(2-吡啶基)-哌嗪(1-PmP)对可乐定(分别为0.25和0.06 mg/kg)诱导的体温过低和运动减少的影响，这两项测试与脑α-肾上腺素能功能有关。1-PmP(腹腔注射1-16 mg/kg)对这两种效应均有剂量依赖性拮抗作用。此外，用丙胺太林(50 mg/kg)预处理可防止丁螺环酮和吉哌隆对可乐定诱导的体温过低的逆转作用。这表明1-PmP可能是丁螺环酮和吉哌隆一些明显的去甲肾上腺素能效应的原因。
