氯乙可乐定揭示了大鼠主动脉中一种非α-肾上腺素能受体的去甲肾上腺素结合位点。
Chloroethylclonidine unmasks a non-alpha-adrenoceptor noradrenaline binding site in the rat aorta.
作者信息
Oriowo M A, Bevan J A
机构信息
Department of Pharmacology, College of Medicine, University of Vermont, Burlington 05405.
出版信息
Eur J Pharmacol. 1990 Mar 20;178(2):243-6. doi: 10.1016/0014-2999(90)90482-l.
The effect of chloroethylclonidine on noradrenaline-induced contractions of the rat aorta was studied. Chloroethylclonidine (1-5 X 10(-5) M) shifted noradrenaline dose-response curve to the right approximately 5000-fold without depressing the maximum. The response to noradrenaline after chloroethylclonidine was not antagonized by phenoxybenzamine (10(-7) M), prazosin (10(-7) M), WB 4101 (10(-7) M) nor yohimbine (10(-5) M) and is therefore not mediated via alpha 1-adrenoceptors. These results would suggest that there is a homogenous population of chloroethylclonidine-sensitive alpha 1-adrenoceptors in the rat aorta and that chloroethylclonidine treatment reveals a non-alpha-adrenoceptor noradrenaline binding site in this tissue.
研究了氯乙可乐定对去甲肾上腺素诱导的大鼠主动脉收缩的影响。氯乙可乐定（1 - 5×10⁻⁵ M）使去甲肾上腺素剂量 - 反应曲线右移约5000倍，而不降低最大反应。氯乙可乐定处理后对去甲肾上腺素的反应不受苯氧苄胺（10⁻⁷ M）、哌唑嗪（10⁻⁷ M）、WB 4101（10⁻⁷ M）或育亨宾（10⁻⁵ M）的拮抗，因此不是通过α₁ - 肾上腺素能受体介导的。这些结果表明，大鼠主动脉中存在对氯乙可乐定敏感的α₁ - 肾上腺素能受体的同质群体，并且氯乙可乐定处理揭示了该组织中一个非α - 肾上腺素能受体的去甲肾上腺素结合位点。
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