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大鼠冠状动脉小动脉中胰淀素对降钙素基因相关肽1（CGRP(1)）受体的非竞争性拮抗作用。

Non-competitive antagonism of amylin on CGRP(1)-receptors in rat coronary small arteries.

作者信息

Sheykhzade M, Nyborg N C

机构信息

Department of Pharmacology, The Royal Danish School of Pharmacy, Universitetsparken 2, DK-2100 Copenhagen O, Denmark.

出版信息

Br J Pharmacol. 2000 May;130(2):386-90. doi: 10.1038/sj.bjp.0703316.

DOI:10.1038/sj.bjp.0703316

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1572076/

Abstract

We examined the interaction between rat-amylin and relaxations induced by rat-alphaCGRP and isoprenaline in rat isolated coronary small arteries. Amylin, 0.1 - 100 nM, had a concentration dependent non-competitive antagonistic effect on rat-alphaCGRP-induced responses with an EC(50) of approximately 1 nM. Amylin did not affect the relaxations induced by isoprenaline at a concentration of 10 nM. The apparent equilibrium dissociation constant, K(A), for CGRP(1)-receptors in the rat coronary small arteries was approximately 2 nM. Analysis of the relationship between receptor occupancy and response to rat-alphaCGRP indicates that the receptor reserve is small. Our results show that amylin in low concentrations acts as a selective non-competitive inhibitor at CGRP(1)-receptors in rat isolated coronary small arteries.

摘要

我们研究了大鼠胰岛淀粉样多肽与大鼠α降钙素基因相关肽（αCGRP）及异丙肾上腺素在大鼠离体冠状动脉小动脉中诱导的舒张反应之间的相互作用。浓度为0.1 - 100 nM的胰岛淀粉样多肽对大鼠αCGRP诱导的反应具有浓度依赖性非竞争性拮抗作用，半数有效浓度（EC50）约为1 nM。浓度为10 nM的胰岛淀粉样多肽不影响异丙肾上腺素诱导的舒张反应。大鼠冠状动脉小动脉中CGRP（1）受体的表观平衡解离常数K（A）约为2 nM。对受体占有率与大鼠αCGRP反应之间关系的分析表明，受体储备较小。我们的结果表明，低浓度的胰岛淀粉样多肽在大鼠离体冠状动脉小动脉的CGRP（1）受体上作为选择性非竞争性抑制剂起作用。