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Investigations of the subtype of α 2 ‐adrenoceptor mediating contractions of the human saphenous vein
Author(s) -
Smith Karen,
Connaughton Sonia,
Docherty James R.
Publication year - 1992
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1992.tb14354.x
Subject(s) - ligand (biochemistry) , binding site , vein , antagonist , potency , chemistry , receptor , stereochemistry , medicine , pharmacology , biology , biochemistry , in vitro
1 We have examined the effects of a series of α 2 ‐adrenoceptor antagonists against isometric contractions to noradrenaline in human saphenous vein, and correlated these potencies with affinities for the α 2A ‐ligand binding site of human platelet and the α 2B ‐ligand binding site of rat kidney. 2 The α 2B ‐selective adrenoceptor antagonists, prazosin, ARC 239 and HV 723 showed high, and the α 2A ‐selective antagonist BRL 44408 showed low, potency in human saphenous vein. 3 Potency in human saphenous vein correlated better with affinity for the α 2B ‐ligand binding site ( r =0.71, n = 12, P < 0.01) than with affinity for the α 2A ‐ligand binding site ( r = 0.56, n = 12, non significant). 4 It is concluded that the postjunctional α 2 ‐adenoceptor of human saphenous vein resembles an α 2B ‐ligand binding site more than an α 2A ‐ligand binding site.