Treatments for obesity and methods for identifying compounds useful for treating obesity
申请人:Pfizer Inc.
公开号:US06451783B1
公开(公告)日:2002-09-17
The present invention provides a method of treating obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the step of administering to a patent having or at risk of having one of the above-mentioned diseases a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors.
本发明提供了一种治疗肥胖症、性功能障碍(包括勃起功能障碍)、糖尿病、
胰岛素抵抗、高
胰岛素血症、X综合症、肾上腺功能障碍、高血压、高
胆固醇血症、动脉硬化、高脂蛋白血症、高
甘油三酯血症或物质滥用的方法,其中所述方法包括向患有或有患上上述疾病风险的患者施用一种治疗有效量的化合物,该化合物减弱了类似鼠标肥胖相关蛋白与
黑色素皮质素受体的结合,但不减弱α-
黑色素细胞刺激素与
黑色素皮质素受体的结合。本发明还提供了一种用于治疗或预防肥胖症、性功能障碍(包括勃起功能障碍)、糖尿病、
胰岛素抵抗、高
胰岛素血症、X综合症、肾上腺功能障碍、高血压、高
胆固醇血症、动脉硬化、高脂蛋白血症、高
甘油三酯血症或物质滥用的化合物的识别方法,该方法包括以下步骤:1)确定化合物是否影响类似鼠标肥胖相关蛋白与
黑色素皮质素受体的结合;2)确定化合物是否影响α-
黑色素细胞刺激素与
黑色素皮质素受体的结合;3)选择减弱类似鼠标肥胖相关蛋白与
黑色素皮质素受体的结合,但不影响α-
黑色素细胞刺激素与
黑色素皮质素受体的结合的化合物。