Abstract
The relationship between α 2-adrenoceptor occupancy and contractile response for B-HT 933 was investigated in canine saphenous vein. B-HT 933 produced a concentration-dependent, α 2-adrenoceptor mediated contractile response in canine saphenous vein with an ED 50 of 0.65 μM. The dissociation constant (K A) of B-HT 933 was calculated to be 5 μM. The relationship between α 2-adrenoceptor occupancy and contractile response for B-HT 933 in canine saphenous vein was hyperbolic, typical of full agonists or agonists with high intrinsic efficacies. B-HT 933 produced a half-maximal response in canine saphenous vein at only 11% α 2-adrenoceptor occupancy, with a maximal response being obtained with 40–60% α 2-adrenoceptor occupancy. We conclude that the selective α 2-adrenoceptor agonist, B-HT 933, has high efficacy at α 2-adrenoceptors, such that a significant α 2-adrenoceptor reserve, or spare α 2-adrenoceptors, exists for this compound in canine saphenous vein.
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