4-Substituted anilides as selective melatonin MT2 receptor agonists |
| |
| Authors: | Epperson James R Deskus Jeffrey A Gentile Anthony J Iben Lawrence G Ryan Elaine Sarbin Nathan S |
| |
| Institution: | Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492-7660, USA. james.epperson@bms.com |
| |
| Abstract: | A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2) binding affinity and MT(2) selectivity of at least 70-fold over the MT(1) receptor. Compound 26 demonstrated full agonism at the MT(2) receptor. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
