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[鸡胚羊膜中α和β肾上腺素能受体的药代动力学分析]

[Pharmacokinetic analysis of alpha- and beta-adrenoreceptors in the chick embryo amnion].

作者信息

Boĭko O V, Manukhin B N

机构信息

Institute of Developmental Biology of the Russian Acad. of Vavilova St., 26.

出版信息

Ross Fiziol Zh Im I M Sechenova. 2000 Oct;86(10):1237-45.

Abstract

Following a stimulation with acetylcholine, the beta-adrenergic agonists adrenaline (A), noradrenaline (NA), isoproterenol (Iso) and salbutamol (Sal) induced a concentration-dependent decrease in the tone and (or) rate of amnion contraction with EC50 ISO < NA << A < Sal. Metaprolol, a specific beta 1-antagonist, induced a rightward shift in the dose-response curves of Iso, NA and A, whereas beta-antagonist butoxamine was ineffective. pA2 values for beta-antagonists were propranolol 8.3, metoprolol 7.0, butoxamine 5.6. EC50 values of alpha-adrenergic agonists form a sequence: clonidine < NA << methoxamine < phenylephrine. Specific alpha-antagonists yohimbine and idazoxan were found to antagonise competitively the effects of NA. The data obtained characterize the adrenergic receptors mediating stimulation of amniotic contractile activity as alpha 2-adrenergic receptors. Inhibition of contractile receptors in amnion is mainly mediated by beta 1-adrenergic receptor activation.

摘要

在用乙酰胆碱刺激后,β-肾上腺素能激动剂肾上腺素(A)、去甲肾上腺素(NA)、异丙肾上腺素(Iso)和沙丁胺醇(Sal)可引起羊膜收缩张力和(或)频率呈浓度依赖性降低,其半数有效浓度(EC50)顺序为Iso < NA << A < Sal。特异性β1拮抗剂美托洛尔可使Iso、NA和A的剂量-反应曲线右移,而β拮抗剂布托沙明则无效。β拮抗剂的pA2值分别为普萘洛尔8.3、美托洛尔7.0、布托沙明5.6。α-肾上腺素能激动剂的EC50值顺序为:可乐定 < NA << 甲氧明 < 去氧肾上腺素。发现特异性α拮抗剂育亨宾和咪唑克生可竞争性拮抗NA的作用。所获得的数据表明,介导羊膜收缩活性刺激的肾上腺素能受体为α2-肾上腺素能受体。羊膜中收缩受体的抑制主要由β1-肾上腺素能受体激活介导。

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