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鸟苷三磷酸增加气道毒蕈碱拮抗剂结合位点:一种受镁离子调节的效应。

GTP increases airway muscarinic antagonist binding sites: an effect regulated by Mg2+.

作者信息

Cheng J B, Townley R G

出版信息

Eur J Pharmacol. 1983 Mar 25;88(2-3):269-72. doi: 10.1016/0014-2999(83)90017-1.

Abstract

Using [3H]QNB, we demonstrated that GTP and Gpp(NH)p increased muscarinic receptor high affinity sites in bovine tracheal muscle preparations; however, neither the dissociation constant of [3H]QNB binding sites nor pulmonary beta-adrenergic receptor sites was altered. The GTP effect on increasing the receptor sites was relatively small (16%), sensitive (ED50 0.48 microM) and specific (Gpp(NH)p greater than GTP = GDP greater than GMP much greater than ATP). Mg2+ potentiated this increase by up to 94.8%, whereas Na+, K+ and Ca2+ had no such effect.

摘要

使用[3H]QNB,我们证明了GTP和Gpp(NH)p增加了牛气管肌肉制剂中的毒蕈碱受体高亲和力位点;然而,[3H]QNB结合位点的解离常数和肺β-肾上腺素能受体位点均未改变。GTP对增加受体位点的作用相对较小(16%)、敏感(ED50为0.48 microM)且具有特异性(Gpp(NH)p>GTP = GDP>GMP>>ATP)。Mg2+可使这种增加增强高达94.8%,而Na+、K+和Ca2+则无此作用。

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The muscarinic receptors of airway smooth muscle: their characterization in vitro.气道平滑肌的毒蕈碱受体:其体外特性研究
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