Antagonist like action of synthetic alpha 2-adrenoceptor agonists on contractile response to catecholamines in smooth muscle strips isolated from rainbow trout stomach (Salmo gairdneri).

T Kitazawa, N Miyashita, A Chugun, K Temma, H Kondo
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Abstract

1. The effects of some synthetic alpha 2-adrenoceptor agonists on the mechanical activity and on contractile responses to catecholamines were examined in smooth muscle strips isolated from rainbow trout stomach. 2. Contractile responses to noradrenaline and adrenaline in the rainbow trout stomach strips were due to alpha 2-adrenoceptor activation. 3. Clonidine, p-aminoclonidine, naphazoline and guanabenz caused no mechanical response but concentration-dependently inhibited the contractile responses to noradrenaline and adrenaline without affecting the responses to acetylcholine, carbachol, 5-hydroxytryptamine and methionine-enkephalin. The order of potency was naphazoline greater than p-aminoclonidine greater than clonidine greater than guanabenz. 4. It is suggested that in the smooth muscle preparation of the trout stomach, some synthetic compounds (clonidine, p-aminoclonidine, naphazoline and guanabenz), which act on mammalian preparations as alpha 2-adrenoceptor agonists, show an antinoradrenaline (-adrenaline) effect; those compounds can be classified as alpha 2-adrenoceptor antagonists.

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合成- 2-肾上腺素能受体激动剂对虹鳟胃平滑肌条对儿茶酚胺收缩反应的拮抗作用。
1. 用虹鳟鱼胃平滑肌条研究了合成α 2-肾上腺素受体激动剂对其机械活性和对儿茶酚胺的收缩反应的影响。2. 虹鳟鱼胃条对去甲肾上腺素和肾上腺素的收缩反应是由于α 2-肾上腺素受体的激活。3.可乐定、对氨基可乐定、萘唑啉和胍那苯对去甲肾上腺素和肾上腺素无机械反应,但浓度依赖性地抑制了去甲肾上腺素和肾上腺素的收缩反应,而不影响乙酰胆碱、氨基酚、5-羟色胺和蛋氨酸-脑啡肽的反应。效价顺序为萘唑啉>对氨基可乐定>可乐定>胍那苯。4. 提示在鳟鱼胃平滑肌制剂中,一些合成化合物(可乐定、对氨基可乐定、萘唑啉和胍那苯)作为α 2-肾上腺素受体激动剂作用于哺乳动物制剂,表现出抗肾上腺素(-肾上腺素)的作用;这些化合物可归类为- 2肾上腺素受体拮抗剂。
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