| Literature DB >> 19041301 |
Michela Buccioni1, Meenakshisundaram Kandhavelu, Piero Angeli, Gloria Cristalli, Diego Dal Ben, Dario Giardinà, Catia Lambertucci, Carmen Lammi, Rosaria Volpini, Gabriella Marucci.
Abstract
Contraction of rat epididymal vas deferens is regulated via a release of neurotransmitters from autonomic nerves and is mediated by alpha(1)-adrenoceptors. This study was directed to the characterization of alpha(1)-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 beta-chloroethyamines, 1 and 2. The antagonist activity of known subtype-selective alpha(1)-adrenoceptor antagonists, WB4101, 5-MU, and RS17053 (alpha(1A)), (+)-cyclazosin (alpha(1B)), and BMY7378 (alpha(1D)), was evaluated in the alpha(1)-adrenoceptors of the studied tissue as such and after pre-treatment with a proper discriminating concentration of beta-chloroetylamines 1 and 2, comparing the results with the affinities determined in classical Wistar rat models: prostatic vas deferens (alpha(1A)), spleen (alpha(1B)), and thoracic aorta (alpha(1D)). The results suggested that two alpha(1A)-adrenoceptors are involved in the contraction of the epididymal vas deferens of young CD rats. These may represent two alpha(1A)-adrenoceptor isoforms that are selectively and irreversibly blocked by beta-chloroetylamines 1 and 2, and reversibly antagonized by RS17053. The minor population, preferentially blocked by 1, seems correspond to a classical alpha(1A)-adrenoceptor subtype, while the major population, preferentially blocked by 2 and antagonized by RS17053 with low affinity, seems to correspond to an alpha(1L)-adrenoceptor.Entities:
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Year: 2008 PMID: 19041301 DOI: 10.1016/j.ejphar.2008.10.067
Source DB: PubMed Journal: Eur J Pharmacol ISSN: 0014-2999 Impact factor: 4.432