科研之友
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摘要
Introduction: The cyclic neuropeptide melanin-concentrating hormone (MCH) shows appetite-stimulating effects indicating an involvement in obesity. Large efforts have been invested in discovery programs to identify novel MCH1 receptor (MCHR1) antagonists. Other indications where MCHR1 antagonists may have a potential use include: anxiety/depression and, more recently, inflammatory responses in the gastrointestinal tract. Areas covered: The current review covers the patent literature on MCHR1 antagonists published from November 2010 to March 2014. The applications have been grouped by filing company, and weight has been put on commenting compounds with disclosed in vivo biological data. Expert opinion: Achieving sufficient separation of the human EtheR-a-Go-go channel has prevented many programs from reaching the clinic. For clinical programs, CNS exposure seems to have been a major challenge. Although clinical studies of MCHR1 antagonists have not been able to conclusively evaluate the concept, the body of evidence suggesting a role for MCHR1 antagonists in weight management is strong and novel chemical series still appear in the patent literature. An MCHR1 antagonist with the appropriate physical chemical properties is needed to convincingly evaluate the MCHR1 concept for obesity treatment and, as knowledge from previous programs are shared, the discovery of such a compound should be achievable.
- 出版日期2015-2
