Agonist pharmacology at recombinant α1A- and α1L-adrenoceptors and in lower urinary tract α1-adrenoceptors

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Phenotype pharmacology of lower urinary tract α(1)-adrenoceptors.

α(1)-Adrenoceptors are involved in numerous physiological functions, including micturition. However, the pharmacological profile of the α(1)-adrenoceptor subtypes remains controversial. Here, we review the literature regarding α(1)-adrenoceptors in the lower urinary tract from the standpoint of α(1L) phenotype pharmacology. Among three α(1)-adrenoceptor subtypes (α(1A), α(1B) and α(1D)), α(1a)-...

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Cardiac α1-adrenoceptor stimulation elicits a positive inotropic effect because of myofilament Ca2+ sensitization with a small increase in Ca2+ transients predominantly mediated by α1B-adrenoceptors via the intracellular alkalinization and potential myosin light chain 2 phosphorylation. However, the α1-adrenoceptor– mediated inotropy exhibits a wide range of species-dependent variation. In addi...

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Dimerization of α1-adrenoceptors

Three distinct genes encode α1-adrenoceptors. Although homodimers of each subtype have been reported, certain but not all combinations of heterodimers of the α1-adrenoceptors appear to form. Key studies in this field are reviewed and the approaches that have been applied to monitoring the selectivity and the basis of α1-adrenoceptor dimerization are discussed. Introduction GPCRs (G-protein-coup...

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Cardiac α1-Adrenoceptors and Inotropy

Cardiac α1-adrenoceptor stimulation elicits a positive inotropic effect because of myofilament Ca2+ sensitization with a small increase in Ca2+ transients predominantly mediated by α1B-adrenoceptors via the intracellular alkalinization and potential myosin light chain 2 phosphorylation. However, the α1-adrenoceptor– mediated inotropy exhibits a wide range of species-dependent variation. In addi...

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Cardiac α1-Adrenoceptors and Inotropy

Cardiac α1-adrenoceptor stimulation elicits a positive inotropic effect because of myofilament Ca2+ sensitization with a small increase in Ca2+ transients predominantly mediated by α1B-adrenoceptors via the intracellular alkalinization and potential myosin light chain 2 phosphorylation. However, the α1-adrenoceptor– mediated inotropy exhibits a wide range of species-dependent variation. In addi...

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ژورنال

عنوان ژورنال: British Journal of Pharmacology

سال: 2013

ISSN: 0007-1188

DOI: 10.1111/bph.12403