Non‐competitive antagonism of amylin on CGRP1‐receptors in rat coronary small arteries
Open Access
- 1 May 2000
- journal article
- Published by Wiley in British Journal of Pharmacology
- Vol. 130 (2) , 386-390
- https://doi.org/10.1038/sj.bjp.0703316
Abstract
We examined the interaction between rat‐amylin and relaxations induced by rat‐αCGRP and isoprenaline in rat isolated coronary small arteries. Amylin, 0.1–100 nM, had a concentration dependent non‐competitive antagonistic effect on rat‐αCGRP‐induced responses with an EC50 of approximately 1 nM. Amylin did not affect the relaxations induced by isoprenaline at a concentration of 10 nM. The apparent equilibrium dissociation constant, KA, for CGRP1‐receptors in the rat coronary small arteries was approximately 2 nM. Analysis of the relationship between receptor occupancy and response to rat‐αCGRP indicates that the receptor reserve is small. Our results show that amylin in low concentrations acts as a selective non‐competitive inhibitor at CGRP1‐receptors in rat isolated coronary small arteries. British Journal of Pharmacology (2000) 130, 386–390; doi:10.1038/sj.bjp.0703316Keywords
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