Abstract：
:To shed light on the discrepancy between reported binding and functional affinity and selectivity at alpha(1b/B)-adrenoceptors, the antagonist (+)-cyclazosin was reinvestigated in rat and rabbit tissues. It displayed a competitive antagonism at alpha(1A) and alpha(1D)-adrenoceptors of rat prostatic vas deferens and aorta with pA(2) values 7.75 and 7.27, respectively. In rabbit thoracic aorta (+)-cyclazosin competitively antagonized noradrenaline-induced contractions at alpha(1B)-adrenoceptors with a pA(2) value of 8.85, whereas its affinity at alpha(1L)-adrenoceptors was markedly lower (pA(2) = 6.75-7.09). In conclusion, these data confirmed that (+)-cyclazosin is a selective alpha(1B)-adrenoceptor antagonist also in functional assays, showing 13- and 38-fold selectivity for the alpha(1B)-adrenoceptor over alpha(1A)- and alpha(1D)-subtypes, respectively. Furthermore, (+)-cyclazosin displayed a significant selectivity for alpha(1B)-adrenoceptors relative to the alpha(1L)-subtype.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Marucci G,Angeli P,Buccioni M,Gulini U,Melchiorre C,Sagratini G,Testa R,Giardinà Ddoi
10.1016/j.ejphar.2005.08.044keywords:
subject
Has Abstractpub_date
2005-10-17 00:00:00pages
100-7issue
1-3eissn
0014-2999issn
1879-0712pii
S0014-2999(05)00898-8journal_volume
522pub_type
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journal_title：European journal of pharmacology
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