期刊
EUROPEAN JOURNAL OF PHARMACOLOGY
卷 605, 期 1-3, 页码 53-56出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejphar.2008.12.044
关键词
Muscarinic M-1 receptor; Ectopic; Orthosteric; Muscarinic M1-preferring agonists
In functional assay assessments using the five muscarinic receptor subtypes, a second generation of muscarinic M-1-preferring receptor agonists [AC-42 (1), AC-260584 (2), 77-LH-28-1 (3) and LY-593039 (4)] was shown to have higher selectivity for muscarinic M-1 over M-3 receptor as compared to historical agonists [talsaclidine (8), sabcomeline (10), xanomeline (11), WAY-132983 (12), cevimeline (9) and NGX-267 (6)]. Another striking difference of these more recent compounds is their affinities for the dopamine D-2 and 5-HT2B receptors. Taken together, these results suggest that the newer compounds may have a greater clinical safety profile, especially with regard to muscarinic M-3 receptor-mediated events, than the historical agonists, but their affinities for other receptors may still compromise their use to validate the therapeutic potential of muscarinic M-1 receptor agonists. (C) 2009 Elsevier B.V. All rights reserved.
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