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

Research output: Contribution to journalArticle

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

Fingerprint

Adrenergic Receptors
Aorta
Ligands
Phenylephrine
Radioligand Assay
CGP 12177
Membranes

Keywords

  • a1-adrenoceptors
  • ß-adrenoceptors

Cite this

@article{72217ed4832b44478cc8a3f807999a1e,
title = "a1-Adrenoceptor antagonist properties of CGP 12177A and other {\ss}-adrenoceptor ligands: evidence against {\ss}3- or atypical {\ss}-adrenoceptors in rat aorta",
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 {\ss}3-adrenoceptors or atypical {\ss}-adrenoceptors.",
keywords = "a1-adrenoceptors, {\ss}-adrenoceptors",
author = "Nataraj Brahmadevara and Shaw, {Angus M.} and Allan MacDonald",
note = "Originally published in: British Journal of Pharmacology (2002), 142 (4), pp.781-787.",
year = "2004",
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language = "English",
journal = "British Journal of Pharmacology",
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a1-Adrenoceptor antagonist properties of CGP 12177A and other ß-adrenoceptor ligands: evidence against ß3- or atypical ß-adrenoceptors in rat aorta. / Brahmadevara, Nataraj; Shaw, Angus M.; MacDonald, Allan.

In: British Journal of Pharmacology, 01.06.2004.

Research output: Contribution to journalArticle

TY - JOUR

T1 - a1-Adrenoceptor antagonist properties of CGP 12177A and other ß-adrenoceptor ligands: evidence against ß3- or atypical ß-adrenoceptors in rat aorta

AU - Brahmadevara, Nataraj

AU - Shaw, Angus M.

AU - MacDonald, Allan

N1 - Originally published in: British Journal of Pharmacology (2002), 142 (4), pp.781-787.

PY - 2004/6/1

Y1 - 2004/6/1

N2 - 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.

AB - 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.

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KW - ß-adrenoceptors

M3 - Article

JO - British Journal of Pharmacology

JF - British Journal of Pharmacology

SN - 0007-1188

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