The a1-adrenoceptor antagonist properties of the ß-adrenoceptor nonconventional partial agonist, CGP 12177A, was investigated in functional assays in rat aorta and in radioligand binding assays in rat cerebral cortical membranes. In addition, binding affinities of other ß-adrenoceptor ligands were measured to investigate any correlation between a1-adrenoceptor affinity and relaxant potency in phenylephrine-constricted rings. This study found that relaxant effects of CGP 12177A and other ß-adrenoceptor ligands in phenylephrine-constricted rat aorta can be attributed to a1-adrenoceptor blockade and are unrelated to effects at ß3-adrenoceptors or atypical ß-adrenoceptors.
|Journal||British Journal of Pharmacology|
|Publication status||Published - 1 Jun 2004|