a1-Adrenoceptor antagonist properties of CGP 12177A and other ß-adrenoceptor ligands: evidence against ß3- or atypical ß-adrenoceptors in rat aorta

Nataraj Brahmadevara, Angus M. Shaw, Allan MacDonald

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Abstract

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.

Original languageEnglish
JournalBritish Journal of Pharmacology
Publication statusPublished - 1 Jun 2004

Keywords

  • a1-adrenoceptors
  • ß-adrenoceptors

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