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。

Intrinsic activity and effects of guanyl-5'-yl imidodiphosphate, Gpp(NH)p on the affinity of partial agonists to the muscarinic receptor.

作者信息

Takayanagi I, Koike K, Okumura K

出版信息

Eur J Pharmacol. 1984 Mar 16;99(1):107-10. doi: 10.1016/0014-2999(84)90439-4.

DOI:10.1016/0014-2999(84)90439-4

Abstract

The effects of a GTP analogue, guanyl-5'-yl imidodiphosphate, Gpp(NH)p on the inhibition of [3H]3-quinuclidinyl benzilate (QNB) binding by some partial agonists were studied with a microsomal fraction of longitudinal muscle of guinea-pig ileum and compared with the intrinsic activity of the partial agonists which was estimated in the longitudinal muscle of guinea-pig ileum. There was a good correlation between the inhibitory effects of Gpp(NH)p on the affinity of the partial agonists to muscarinic receptors and their intrinsic activity.

摘要

研究了一种鸟苷三磷酸（GTP）类似物——鸟苷 - 5'-亚氨基二磷酸（Gpp(NH)p）对某些部分激动剂抑制豚鼠回肠纵肌微粒体部分[3H]3 - 喹核醇基苯甲酸酯（QNB）结合的作用，并与在豚鼠回肠纵肌中估计的部分激动剂的内在活性进行了比较。Gpp(NH)p对部分激动剂与毒蕈碱受体亲和力的抑制作用与其内在活性之间存在良好的相关性。

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