A Thienopyridazinone-Based Melanin-Concentrating Hormone Receptor 1 Antagonist with Potent in Vivo Anorectic Properties

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 an...

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Veröffentlicht in:	Journal of medicinal chemistry 2006-06, Vol.49 (13), p.3753-3756
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Appetite Depressants - chemical synthesis Appetite Depressants - pharmacokinetics Appetite Depressants - pharmacology Biological and medical sciences Biological Availability Body Weight - drug effects Brain - metabolism Eating - drug effects Half-Life Hormones. Endocrine system Male Medical sciences Obesity - drug therapy Permeability Pharmacology. Drug treatments Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacology Rats Rats, Sprague-Dawley Receptors, Somatostatin - antagonists & inhibitors Stereoisomerism Structure-Activity Relationship Thiophenes - chemical synthesis Thiophenes - pharmacokinetics Thiophenes - pharmacology
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