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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.

DOI:10.1016/0014-2999(83)90017-1
PMID:6852113
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。

相似文献

1
GTP increases airway muscarinic antagonist binding sites: an effect regulated by Mg2+.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。
Eur J Pharmacol. 1983 Mar 25;88(2-3):269-72. doi: 10.1016/0014-2999(83)90017-1.
2
Intrinsic activity and effects of guanyl-5'-yl imidodiphosphate, Gpp(NH)p on the affinity of partial agonists to the muscarinic receptor.鸟苷-5'-亚氨基二磷酸(Gpp(NH)p)的内在活性及其对部分激动剂与毒蕈碱受体亲和力的影响。
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MgCl2-sensitive and Gpp(NH)p-sensitive antagonist binding states of rat heart muscarinic receptors: preferential detection at ambient temperature assay and location in two subcellular fractions.大鼠心脏毒蕈碱受体的MgCl2敏感性和Gpp(NH)p敏感性拮抗剂结合状态:在环境温度测定中优先检测及在两个亚细胞组分中的定位
Mol Cell Biochem. 1990 May 10;94(2):133-46. doi: 10.1007/BF00214120.
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Changes in affinity states during down-regulation of muscarinic receptors in tracheal smooth muscle of organophosphate-treated swine.有机磷处理猪气管平滑肌毒蕈碱受体下调过程中亲和力状态的变化
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J Pharmacol Exp Ther. 1986 May;237(2):419-27.

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