Parle M, Kulkarni S K
Arch Int Pharmacodyn Ther. 1984 Sep;271(1):122-6.
Effect of various concentrations of clonidine (1.875 X 10(-11) to 1.875 X 10(-6) M) was investigated on rectus abdominis muscle of frog. In lower concentrations it neither had any effect per se nor did it alter the contractile effect of acetylcholine. However, a higher concentration of clonidine (1.875 X 10(-6) M) evoked characteristic slow but sustained contractions. Such an effect was not observed with epinephrine, norepinephrine or isoprenaline. Clonidine-induced sustained contractions were resistant to d-tubocurarine (2.545 X 10(-9) M) but susceptible to blockade by yohimbine (5.116 X 10(-8) M), an alpha 2 antagonist, and verapamil (2.04 X 10(-8) M), a calcium channel blocker. Probably activation of post-synaptic alpha 2 adrenoceptors by clonidine was responsible for the observed effect. This is further supported by the observation that guanfacine, a more specific alpha 2 adrenoceptor agonist, also evoked identical, slow and sustained contractions which could be readily reversed by yohimbine.
研究了不同浓度可乐定(1.875×10⁻¹¹至1.875×10⁻⁶M)对青蛙腹直肌的影响。在较低浓度下,它本身既没有任何作用,也没有改变乙酰胆碱的收缩作用。然而,较高浓度的可乐定(1.875×10⁻⁶M)引起了特征性的缓慢但持续的收缩。肾上腺素、去甲肾上腺素或异丙肾上腺素未观察到这种作用。可乐定诱导的持续收缩对筒箭毒碱(2.545×10⁻⁹M)有抗性,但对α₂拮抗剂育亨宾(5.116×10⁻⁸M)和钙通道阻滞剂维拉帕米(2.04×10⁻⁸M)的阻断敏感。可乐定对突触后α₂肾上腺素能受体的激活可能是观察到的效应的原因。胍法辛是一种更特异的α₂肾上腺素能受体激动剂,也引起相同的缓慢且持续的收缩,且能被育亨宾轻易逆转,这一观察结果进一步支持了这一点。