| Literature DB >> 16789729 |
Brian Dyck1, Stacy Markison, Liren Zhao, Junko Tamiya, Jonathan Grey, Martin W Rowbottom, Mingzhu Zhang, Troy Vickers, Katie Sorensen, Christi Norton, Jenny Wen, Christopher E Heise, John Saunders, Paul Conlon, Ajay Madan, David Schwarz, Val S Goodfellow.
Abstract
Melanin-concentrating hormone receptor antagonists containing thieno- and a benzopyridazinone cores were designed and tested as potential anorectic agents. These ligands showed high affinity for the receptor, potent functional activity in vitro, and good oral bioavailabilty in rats. The thiophene analogue exhibited low iv clearance, long half-life, and high brain penetration. In obese rats, the thienopyridazinone demonstrated a dose-dependent reduction in feeding and body weight with doses between 1 and 10 mg kg-1.Entities:
Mesh：
Substances：
Year: 2006 PMID： 16789729 DOI： 10.1021/jm051263c
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446