单胺能系统参与丁螺环酮的药理作用。
Monoaminergic involvement in the pharmacological actions of buspirone.
作者信息
Skolnick P, Weissman B A, Youdim M B
出版信息
Br J Pharmacol. 1985 Nov;86(3):637-44. doi: 10.1111/j.1476-5381.1985.tb08940.x.
Abstract
Buspirone, MJ-13805 and MJ-13653 did not produce a '5-hydroxytryptamine (5-HT) syndrome' in rats at doses up to 20 mg kg-1. These drugs were very weak 5-HT uptake blockers (IC50 much greater than 10 microM) compared to drugs such as chlorimipramine. These drugs did not inhibit either monoamine oxidase (MAO)-A or MAO-B. The Ki values for these agents as inhibitors of [3H]-5-HT and [3H]-ketanserin binding to rat frontal cortex or hippocampal membranes were in the microM range, well above the brain concentrations achieved after an oral dose of 25 mg kg-1. Parenterally administered buspirone blocked apomorphine-induced stereotypy, inhibited the 5-HT syndrome elicited by 5-methoxy-N,N-dimethyltryptamine, and delayed the onset of p-chloroamphetamine induced behaviours.
摘要
在大鼠中，给予高达20mg/kg的剂量时，丁螺环酮、MJ-13805和MJ-13653不会产生“5-羟色胺（5-HT）综合征”。与氯米帕明等药物相比，这些药物是非常弱的5-HT摄取阻滞剂（IC50远大于10μM）。这些药物既不抑制单胺氧化酶（MAO）-A也不抑制MAO-B。这些药物作为[3H]-5-HT和[3H]-酮色林与大鼠额叶皮质或海马膜结合的抑制剂，其Ki值在μM范围内，远高于口服25mg/kg剂量后达到的脑浓度。经胃肠外给药的丁螺环酮可阻断阿扑吗啡诱导的刻板行为，抑制5-甲氧基-N，N-二甲基色胺引发的5-HT综合征，并延迟对氯苯丙胺诱导行为的发作。
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