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Abstract #46130 Published in IGR 13-2
(alpha)2C-adrenoceptor modulators: A patent review
Quaglia W; Del Bello F; Giannella M; Piergentili A; Pigini MExpert Opinion on Therapeutic Patents 2011; 21: 455-481
Introduction: (alpha)2-Adrenoceptors ((alpha)2-ARs) are membrane proteins belonging to the superfamily of GPCRs. Detailed studies have shown three different subtypes, namely (alpha)2A, (alpha)2B and (alpha)2C. Although numerous (alpha)2-AR ligands exist, only a small set of compounds have shown even a degree of selectivity among the three (alpha)2-AR subtypes. Moreover, these compounds suffer from binding to receptor sites outside the (alpha)2-AR subfamily. Efforts made to understand the biological significance of each (alpha)2-AR subtype have greatly been assisted by genetically engineered mice. The main results obtained suggest that (alpha)2C-AR stimulation may represent a therapeutic strategy to get an analgesic response with reduced sedative effects and undesirable changes in blood pressure due to (alpha)2A-AR activation. Areas covered: This review summarizes the patent literature about the development of (alpha)2C-AR modulators from 2000 to early 2010 and their therapeutic effects evoked by the interaction with this receptor subtype. Expert opinion: Over 90 patents have been deposited in the last 10 years regarding different methods of (alpha)2C-AR modulation (use of agonists or antagonists, nucleic acids and polypeptides) for diagnosis, prognosis and treatment of disorders involving this receptor. Nevertheless, despite the numerous published patents, ligands highly selective for the (alpha)2C-AR subtype, which continues to be enigmatic, are lacking.
W. Quaglia. University of Camerino, Via S. Agostino 1, Camerino 62032, Italy. Email: wilma.quaglia@unicam.it
Classification:
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
3.8 Pharmacology (Part of: 3 Laboratory methods)
