Recent patents on novel MCH1 receptor antagonists as potential anti-obesity drugs.

Katalin K Szalai, Gyula Beke, János Éles, Tamás Kitka, Péter Kovács, József Nagy, Sándor Farkas, András Boros
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引用次数: 11

Abstract

Today, the 'obesity pandemic' is one of the biggest health issues around the world. Melanin-concentrating hormone (MCH), a hypothalamic neuropeptide, is one of the most potent, central stimulators of feeding and it also attenuates energy expenditure. Inhibitions of the MCH receptor, the melanin-concentrating hormone receptor-1 (MCHR1), has attracted considerable attention as a potential anti-obesity drug, during the last decade. Now, there are a large number of MCHR1 antagonists, pharmacological tools and clinical drug candidates that can provide clues to develop new structures with high potency and good pharmacokinetic profile. The function of MCHR1 in energy homeostasis, obesity, metabolic syndrome, mood disorders and inflammatory bowel disease is discussed. Relevant clinical trials and patent background information of the MCHR1 antagonists over the last 4 years are also reviewed.

新型MCH1受体拮抗剂作为潜在的抗肥胖药物的最新专利。
如今,“肥胖流行病”是世界上最大的健康问题之一。黑色素浓缩激素(melanin - concentration hormone, MCH)是一种下丘脑神经肽,是最有效的中枢刺激物之一,它还能降低能量消耗。在过去的十年中,抑制MCH受体,即黑色素浓缩激素受体-1 (MCHR1)作为一种潜在的抗肥胖药物引起了相当大的关注。现在,有大量的MCHR1拮抗剂、药理工具和临床候选药物可以为开发高效和良好药代动力学特征的新结构提供线索。讨论了MCHR1在能量稳态、肥胖、代谢综合征、情绪障碍和炎症性肠病中的功能。综述了近4年来MCHR1拮抗剂的相关临床试验和专利背景信息。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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