Receptor binding profile of cyclazosin, a new alpha 1B-adrenoceptor antagonist

  • Eur J Pharmacol. 1995 Dec 4;287(1):13-6. doi: 10.1016/0014-2999(95)00471-7.
D Giardinà  1 ,  M Crucianelli ,  C Melchiorre ,  C Taddei ,  R Testa
Affiliations
  • 1. Department of Chemical Sciences, University of Camerino, Italy.
PMID: 8666020 DOI: 10.1016/0014-2999(95)00471-7
Abstract

The binding profile of cyclazosin, a new prazosin-related Alpha 1-adrenoceptor antagonist, at Alpha 1-, Alpha 2-adrenoceptors, dopamine D2 and 5-HT1A receptors was compared to that of 5-methylurapidil, spiperone, risperidone and other prazosin-related ligands. In addition, cyclazosin was investigated at native and cloned Alpha 1-adrenoceptor subtypes. Cyclazosin showed high specificity for Alpha 1-adrenoceptors and a 10-15-fold selectivity for Alpha 1B (Alpha 1b)-adrenoceptors with respect to the Alpha 1A (Alpha 1a) subtype (pKi values of 9.23-9.57 and 8.18-8.41, respectively). However, it failed to discriminate between cloned Alpha 1b and Alpha 1d-adrenoceptors (pKi values of 9.23 and 9.28, respectively).

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