特异性β3肾上腺素能受体激动剂研究进展

Research progress of specific β3 adrenoceptor agonists

β3肾上腺素受体(β3 adrenoceptor,β3-AR)主要存在于具有产热功能的棕色脂肪细胞和白色脂肪细胞上。β3-AR激动剂通过刺激白色脂肪组织的脂解作用和棕色脂肪组织的产热作用,起到抗肥胖作用;同时通过增加脂肪组织对胰岛素的敏感性和反应性,它在2型糖尿病的治疗中扮演重要角色;此外,β3-AR激动剂具有胃肠道解痉作用及心血管作用。自1983年以来,β3肾上腺素受体激动剂的研制与开发在全世界已引起广泛的重视。目前已鉴定研制的β3肾上腺素受体激动剂有32种,9种尚处于开发阶段,5种处于临床试验阶段,10种已终止研发,8种没有研制报道。β3肾上腺受体激动剂的研制与开发必将为肥胖症和糖尿病的治疗提供新的手段和新思路,具有广阔的前景。

β3 adrenoceptor （β3-AR） is predominantly expressed in white and brown adipose tissue. β3 adrenoceptor agonist stimulates the lipolysis of white adipose tissue and non-shivering thermogenesis of brown adipose tissue to exert its antiobese action. Moreover, β3 adrenoeeptor agonist increases the sensitivity and response of adipose tissue to insulin and it play an important role in the treatment of type 2 diabetes. In addition, β3 adrenoeeptor agonist can also relax gastrointestinal spasm and show cardiovascular effect in human heart and vascular tissues. There has been increasing concerned in the study and development of β3 AR agonists since 1983. Up to date, 32 kinds of β3 AR agonists have been identified. The development of β3 AR agonists can provide new strategy and approach for pharmacotherapy of obesity and diabetic mellitus and will have Spaciously the used out look in the field of medicine.