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Regional distribution and regulation of [125I]calcitonin gene-related peptide binding sites in coronary arteries.

Abstract：

:Quantitative in vitro autoradiographic techniques were used to localize and characterize 125I-labelled human calcitonin gene-related peptide ([125I]hCGRP) binding sites in sections of bovine left anterior descending coronary artery (LAD). Specific high affinity (Kd 0.4 nM) [125I]hCGRP binding sites were localized to the media of both epicardial and myocardial coronary arteries. Binding site density was greater in distal epicardial and myocardial arteries than in proximal epicardial regions of the LAD. Binding sites exhibited a significantly higher affinity for alpha-hCGRP (Ki 1.1 nM) than for hCGRP-(8-37) (Ki 7.0 nM) and [Cys(ACM)2,7]hCGRP (Ki 27.4 nM). Guanosine-5'-O-(3-thiotriphosphate) inhibited [125I]hCGRP binding in a concentration-dependent manner. Extrinsic denervation of the bovine heart resulted in a depletion of CGRP-like immunoreactive perivascular nerve fibres and an increase in the density of coronary artery [125I]hCGRP binding sites (P = 0.0092). The regional distribution of binding sites in human coronary arteries differed from that observed in bovine and porcine vessels. It is concluded that selective, G protein-coupled, CGRP receptors are present in the media of bovine coronary arteries; there are both regional and species differences in the distribution of CGRP binding sites in coronary arteries and endogenous CGRP may exert a tonic influence on coronary vasomotor tone.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Knock GA,Wharton J,Gaer JA,Yacoub MH,Taylor KM,Polak JM

doi

10.1016/0014-2999(92)90483-k

keywords:

subject

Has Abstract

pub_date

1992-09-04 00:00:00

pages

415-25

issue

3

eissn

0014-2999

issn

1879-0712

pii

0014-2999(92)90483-K

journal_volume

219

pub_type

杂志文章

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