公开(公告)号：US20070117827A1

公开(公告)日：2007-05-24

申请号：US11492685

申请日：2006-07-24

申请人： Gary Tollefson ,  Anthony McKinney ,  Michelle Higgin ,  John McCall

发明人： Gary Tollefson ,  Anthony McKinney ,  Michelle Higgin ,  John McCall

IPC分类号： A61K31/485 ,  A61K31/165

CPC分类号： A61K31/137 ,  A61K31/138 ,  A61K31/165 ,  A61K31/485 ,  A61K45/06 ,  A61K2300/00

摘要： Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a metabolite of naltrexone, such as 6-β-naltrexol or a prodrug of a naltrexone metabolite, and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) and/or a melanocortin 4 receptor (MC4-R), and/or increases the concentration of α-MSH in the central nervous system. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity with a metabolite of naltrexone, such as 6-β-naltrexol or a prodrug of a naltrexone metabolite, and treating that individual to enhance α-MSH activity, e.g., by administration of a second compound causes increased agonism of MC3-R and/or MC4-R, and/or increases the concentration of α-MSH in the central nervous system.

摘要翻译： 公开了用于影响体重减轻的组合物，其包含第一化合物和第二化合物，其中第一化合物是纳曲酮的代谢物，例如6-β-纳曲酮或纳曲酮代谢物的前药，并且所述第二化合物导致增加的激动 黑皮质素3受体（MC3-R）和/或黑皮质素4受体（MC4-R），和/或增加中枢神经系统中α-MSH的浓度。 还公开了影响体重减轻，增加能量消耗，增加个体饱腹感或抑制个体食欲的方法，其包括确定有需要的个体，并用纳曲酮代谢物治疗该个体以拮抗阿片受体活性， 作为6-β-纳曲酮或纳曲酮代谢物的前药，并且例如通过施用第二化合物治疗该个体以增强α-MSH活性，导致MC3-R和/或MC4-R的激动作用增加，和/或 增加中枢神经系统中α-MSH的浓度。