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Design and Synthesis of an α 1a ‐Adrenergic Receptor Subtype‐Selective Antagonist from BE2254
Author(s) -
Chiu George,
Gluchowski Charles,
Forray Carlos
Publication year - 2006
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/j.1747-0285.2006.00398.x
Subject(s) - antagonist , potency , chemistry , pharmacology , adrenergic antagonist , adrenergic receptor , receptor , hyperplasia , adrenergic , selectivity , receptor antagonist , stereochemistry , endocrinology , medicine , biochemistry , in vitro , catalysis
An α 1a ‐adrenoceptor‐selective antagonist has the potential to be a new benign prostatic hyperplasia drug with reduced side‐effects. Modification of the non‐selective antagonist BE2254 led to the development of a series of tetralin analogs. Evaluation of these compounds in cloned human α 1 ‐adrenoceptors resulted in the discovery of an analog that showed selectivity toward the human α 1a ‐adrenergic receptor subtype. The compound also showed moderate potency to block human prostate muscle contraction.