Identification of alpha1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens
Articolo
Data di Pubblicazione:
2009
Citazione:
Identification of alpha1-adrenoceptor subtypes involved in contraction of young CD rat epididymal vas deferens / M. Buccioni, M. Kandhavelu, P. Angeli, G. Cristalli, D. Dal Ben, D. Giardinà, C. Lambertucci, C. Lammi, R. Volpini, G. Marucci. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 602:2-3(2009 Jan 14), pp. 388-394. [10.1016/j.ejphar.2008.10.067]
Abstract:
Contraction of rat epididymal vas deferens is regulated via a release of neurotransmitters from autonomic nerves and is mediated by α1-adrenoceptors. This study was directed to the characterization of α1-adrenoceptors involved in the contraction of the epididymal portion of young CD rat vas deferens, that were selectively discriminated in two populations through the irreversible blockade of two β-chloroethyamines, 1 and 2. The antagonist activity of known subtype-selective α1-adrenoceptor antagonists, WB4101, 5-MU, and RS17053 (α1A), (+)-cyclazosin (α1B), and BMY7378 (α1D), was evaluated in the α1-adrenoceptors of the studied tissue as such and after pre-treatment with a proper discriminating concentration of β-chloroetylamines 1 and 2, comparing the results with the affinities determined in classical Wistar rat models: prostatic vas deferens (α1A), spleen (α1B), and thoracic aorta (α1D). The results suggested that two α1A-adrenoceptors are involved in the contraction of the epididymal vas deferens of young CD rats. These may represent two α1A-adrenoceptor isoforms that are selectively and irreversibly blocked by β-chloroetylamines 1 and 2, and reversibly antagonized by RS17053. The minor population, preferentially blocked by 1, seems correspond to a classical α1A-adrenoceptor subtype, while the major population, preferentially blocked by 2 and antagonized by RS17053 with low affinity, seems to correspond to an α1L-adrenoceptor.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
α1-adrenoceptor antagonist; α1-adrenoceptor subtype; β-chloroethyamine; CD rat vas deferens
Elenco autori:
M. Buccioni, M. Kandhavelu, P. Angeli, G. Cristalli, D. Dal Ben, D. Giardinà, C. Lambertucci, C. Lammi, R. Volpini, G. Marucci
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