鸟嘌呤核苷酸诱导的毒蕈碱型胆碱能拮抗剂结合中的正协同性。

Guanine nucleotide-induced positive cooperativity in muscarinic-cholinergic antagonist binding.

作者信息

Boyer J L, Martínez-Cárcamo M, Monroy-Sánchez J A, Posadas C, García-Sáinz J A

出版信息

Biochem Biophys Res Commun. 1986 Jan 14;134(1):172-7. doi: 10.1016/0006-291x(86)90543-7.

DOI:10.1016/0006-291x(86)90543-7

Abstract

The effect of guanine nucleotides on the binding of [3H] Quinuclidinyl benzilate to heart muscarinic receptors was studied. It was observed that GTP and Gpp (NH)p increased antagonist binding. Scatchard transformation of the data resulted in curvilinear plots (downward concavity) consistent with positive cooperativity. Graphic analysis for cooperativity indicated that guanine nucleotides: a) increased slightly but consistently the affinity for the antagonist (independent of receptor occupancy) and b) induce positive cooperativity in the binding of [3H]QNB (dependent of receptor occupancy).

摘要

研究了鸟嘌呤核苷酸对[3H]喹核醇基苯甲酸酯与心脏毒蕈碱受体结合的影响。观察到GTP和Gpp(NH)p增加了拮抗剂的结合。对数据进行Scatchard转换得到与正协同性一致的曲线（向下凹陷）。协同性的图形分析表明，鸟嘌呤核苷酸：a) 对拮抗剂的亲和力略有但持续增加（与受体占有率无关），b) 在[3H]QNB的结合中诱导正协同性（与受体占有率有关）。

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