A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties

…, T Vickers, K Sorensen, C Norton, J Wen…

文献索引：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. Journal of Medicinal Chemistry, 2006 , vol. 49, # 13 p. 3753 - 3756

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被引用次数: 36

摘要

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- ...