ArticleBritish journal of pharmacology2004
ALpha1-adrenoceptor antagonist properties of CGP 12177A and other beta-adrenoceptor ligands: evidence against beta(3)- or atypical beta-adrenoceptors in rat aorta.
Article in British journal of pharmacology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 44 citations in OpenAlex.
- Hypoxia-Dependent Upregulation of VEGF Relies on β3-Adrenoceptor Signaling in Human Retinal Endothelial and Müller Cells.International journal of molecular sciences · 2025Article
- Adrenoceptors in the Lower Urinary Tract.Handbook of experimental pharmacology · 2024Review
- Role of βInternational journal of clinical and experimental pathology · 2017Article
- Cardiac alpha1-adrenergic receptors: novel aspects of expression, signaling mechanisms, physiologic function, and clinical importance.Pharmacological reviews · 2014Review
- Different β-adrenoceptor subtypes coupling to cAMP or NO/cGMP pathways: implications in the relaxant response of rat conductance and resistance vessels.British journal of pharmacology · 2013Article
- Automated imaging reveals a concentration dependent delay in reversibility of cardiac myocyte hypertrophy.Journal of molecular and cellular cardiology · 2012Article
- The role of monoamines in the changes in body temperature induced by 3,4-methylenedioxymethamphetamine (MDMA, ecstasy) and its derivatives.British journal of pharmacology · 2010Review
- Beta 3-adrenoreceptor regulation of nitric oxide in the cardiovascular system.Journal of molecular and cellular cardiology · 2010Review
- Subtypes of functional alpha1-adrenoceptor.Cellular and molecular life sciences : CMLS · 2010Review
- Role of alpha 1- and beta 3-adrenoceptors in the modulation by SR59230A of the effects of MDMA on body temperature in the mouse.British journal of pharmacology · 2009Article
- Modelling of alpha1-adrenoceptor-mediated temporal dynamics of inotropic response in rat heart to assess ligand binding and signal transduction parameters.British journal of pharmacology · 2009Article
- Nuclear alpha1-adrenergic receptors signal activated ERK localization to caveolae in adult cardiac myocytes.Circulation research · 2008Article
- Tools to study beta3-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2007Review
- beta-adrenoceptor mediated responses in rat pulmonary artery: putative role of TASK-1 related K channels.Naunyn-Schmiedeberg's archives of pharmacology · 2006Article
- Mixed beta3-adrenoceptor agonist and alpha1-adrenoceptor antagonist properties of nebivolol in rat thoracic aorta.British journal of pharmacology · 2006Article
- Direct demonstration of beta1- and evidence against beta2- and beta3-adrenoceptors, in smooth muscle cells of rat small mesenteric arteries.British journal of pharmacology · 2005Article
- Positive inotropic and lusitropic effects mediated via the low-affinity state of beta1-adrenoceptors in pithed rats.British journal of pharmacology · 2005Article
- Role of beta2-adrenoceptors (beta-AR), but not beta1-, beta3-AR and endothelial nitric oxide, in beta-AR-mediated relaxation of rat intrapulmonary artery.Naunyn-Schmiedeberg's archives of pharmacology · 2005Article
- Comparison of the alpha-adrenoceptor-mediated effects of beta3-adrenoceptor ligands in rat pulmonary artery.Naunyn-Schmiedeberg's archives of pharmacology · 2005Article
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3 authors at 1 institution in 1 country.
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Abstract
1. The alpha(1)-adrenoceptor antagonist properties of the beta-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 beta-adrenoceptor ligands were measured to investigate any correlation between alpha(1)-adrenoceptor affinity and relaxant potency in phenylephrine-constricted rings. 2. In functional studies, CGP 12177A produced parallel rightward shifts of the phenylephrine CRC with no reduction in the maximum responses. Schild regression analysis gave a straight line with a slope of 0.95 (95% CL: 0.87-1.04), suggesting reversible competitive antagonism, and gave a pK(B) value of 5.26. In contrast, CGP 12177A (<or=300 microm) had no effect on contraction induced by the thromboxane-mimetic, U46619. 3. In binding studies, CGP 12177A competed monophasically with [(3)H]prazosin binding (Hill slope, 0.95, 95% CL: 0.76-1.13), giving a pK(i) value of 5.48, in good agreement with the pK(B) from functional studies. 4. Competition experiments with various other beta-adrenoceptor ligands showed that they all displaced [(3)H]prazosin in a manner consistent with one-site competition. pK(i) values were as follows: SR 59230A, 6.25; cyanopindolol, 6.33; bupranolol, 6.35; alprenolol, 5.90; propranolol, 5.80; BRL 37344, 5.50; ICI 118551, 5.55; CGP 20712A, 5.26. The pK(i) values correlated well with the pEC(50) values for relaxation of phenylephrine-constricted rat aorta obtained previously (r(2)=0.984, P<0.0001). 5. In conclusion, relaxant effects of CGP 12177A and other beta-adrenoceptor ligands in phenylephrine-constricted rat aorta can be attributed to alpha(1)-adrenoceptor blockade and are unrelated to effects at beta(3)-adrenoceptors or atypical beta-adrenoceptors.
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