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An evaluation of the ability of a series of full alpha-1 adrenoceptor agonists to release internal calcium in venous smooth muscle

KF Jim, RA Macia and WD Matthews

Our previous studies have shown that activation of postsynaptic alpha-2 adrenoceptors mainly utilizes extracellular calcium whereas activation of postsynaptic alpha-1 adrenoceptors mobilizes both extracellular and intracellular calcium to produce contractions in the canine saphenous vein. In the present study, the abilities of several full alpha-1 adrenoceptor agonists to release internal calcium for contractions in the canine saphenous vein were evaluated. Contractions to these alpha-1 agonists at two different equieffective concentrations (concentrations that produced 50 and 80% of the maximum phenylephrine response, PE50 and PE80, respectively) were determined in both zero external calcium medium and in normal calcium medium containing 5 mM La . If a correlation exists between the efficacy of an agonist and its ability to release internal Ca++, the contractile response to each agonist should be similar under these conditions. The results indicated marked variations in mechanical responses elicited by these alpha-1 agonists at both PE50 and PE80 concentrations. The data suggest a lack of correlation between efficacy and the ability to release internal calcium to induce contractions for a series of full alpha-1 adrenoceptor agonists in venous smooth muscle.

Volume 235, Issue 2, pp. 377-381, 11/01/1985
Copyright © 1985 by American Society for Pharmacology and Experimental Therapeutics




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Copyright © 1985 by the American Society for Pharmacology and Experimental Therapeutics.