Abstract：
A specific type of beta-adrenergic receptor was discovered in the decade of 1980s and subsequently recognized as a new type of beta-adrenergic receptor, called beta3-adrenoceptor (β3-AR). β3-AR expresses in different tissues, including adipose tissue, gall bladder, stomach, small intestine, cardiac myocytes, urinary bladder, and brain. Structurally, β3-AR is very similar to β1- and β2-AR and belongs to a G-protein coupled receptor that uses cAMP as an intracellular second messenger. Alternatively, it also activates the NO-cGMP cascade. Stimulation of the β3-AR increases lipolysis, fatty acid oxidation, energy expenditure, and insulin action, leading to anti-obesity and anti-diabetic activity. Moreover, β3-AR differentially regulates the myocardial contraction and relaxes the urinary bladder to balance the cardiac activity and delay the micturition reflex, respectively. In recent years, this receptor has served as an attractive target for the treatment of obesity, type 2 diabetes, congestive heart failure, and overactive bladder syndrome. Several β3-AR agonists are in the emerging stage that can exert novel pharmacological benefits in different therapeutic areas. The present review focuses on the structure, signaling, physiological, and metabolic activities of β3-AR. Additionally, therapeutic approaches of β3-AR have also been considered.
摘要：
在1980年代的十年中发现了一种特定类型的β-肾上腺素能受体，随后被认为是一种新型的β-肾上腺素能受体，称为β3-肾上腺素受体（β3-AR）。β3-AR在不同组织中表达，包括脂肪组织,胆囊,胃,小肠,心肌细胞,膀胱,和大脑。在结构上,β3-AR与β1-和β2-AR非常相似，属于使用cAMP作为细胞内第二信使的G蛋白偶联受体。或者，它还激活NO-cGMP级联。刺激β3-AR增加脂解，脂肪酸氧化，能量消耗，和胰岛素的作用，导致抗肥胖和抗糖尿病活性。此外，β3-AR差异调节心肌收缩和松弛膀胱以平衡心脏活动和延迟排尿反射，分别。近年来,这种受体已经成为治疗肥胖症的一个有吸引力的靶点，2型糖尿病,充血性心力衰竭,膀胱过度活动症.几种β3-AR激动剂处于新兴阶段，可以在不同的治疗领域发挥新的药理学益处。本审查的重点是结构，信令,生理,和β3-AR的代谢活性。此外,β3-AR的治疗方法也已被考虑。
