868662-16-2Relevant academic research and scientific papers
A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties
Dyck, Brian,Markison, Stacy,Zhao, Liren,Tamiya, Junko,Grey, Jonathan,Rowbottom, Martin W.,Zhang, Mingzhu,Vickers, Troy,Sorensen, Katie,Norton, Christi,Wen, Jenny,Heise, Christopher E.,Saunders, John,Conlon, Paul,Madan, Ajay,Schwarz, David,Goodfellow, Val S.
, p. 3753 - 3756 (2007/10/03)
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 bioavailability 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.
2- (3-AMINOPYRROLIDIN-1-YL) PYRIDINES AS MELANIN-CONCENTRATING HORMONE RECEPTOR AN TAGONISTS
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Page/Page column 38, (2010/02/14)
Melanin-concentrating hormone (MCH) receptor antagonists are disclosed having utility for the treatment of MCH receptor-based disorders such as obesity. The compounds of this invention have the following structure: including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, Het, X and Cyc are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.
