《生命科学》 2014, 26(11): 1200-1206

乳酸受体GPR81的研究进展

赵乃倩1，荣青峰1，郭　娜1，张　策2*

(1 山西医科大学第二医院老年病科，太原 030001；2 山西医科大学生理学教研室，太原 030001)

摘　要：摘　要：GPR81 是乳酸的特异性受体，具有调节脂肪细胞发育和分化、抑制脂肪分解、抑制炎性反应，以及调节脑能量代谢、脑血流量和神经元功能的协同变化等生物学功能。GPR81 生物学功能的分子机制包括：(1) 通过GPR81/Gi/cAMP 信号转导通路抑制脂肪分解和调节脑能量代谢、脑血流量和神经元功能的协同变化；(2) 通过GPR81/β-arrestin 2/NF-κB 及GPR81/β-arrestin 2/NLRP3 信号通路抑制巨噬细胞炎性反应。GPR81 功能异常与肥胖、血脂异常、胰岛素抵抗、糖耐量减低和2 型糖尿病密切相关，还可能参与了颞叶癫痫、中枢性疲乏及缺血性脑血管疾病的发生发展。就乳酸受体GPR81 在脂质代谢、炎性反应及中枢神经系统中的作用进行综述。

Progress in lactate receptor GPR81

ZHAO Nai-Qian1， RONG Qing-Feng1， GUO Na1， ZHANG Ce2*

(1 Department of Geriatrics， Second Hospital of Shanxi Medical University， Taiyuan 030001， China;
    2 Department of Physiology， Shanxi Medical University， Taiyuan 030001， China)

Abstract: Abstract: GPR81 functions as a specific receptor for glycolytic metabolite 2-hydroxy-propionic acid (lactate) and mediates various physiological roles such as the regulation of adipocyte development and differentiation， antilipolytic effects， anti-inflammatory effects and the coordinated regulation of brain energy metabolism， cerebral blood flow， and neuronal function. GPR81 exerts its physiological functions by two different mechanisms， one by Gi-type G protein-dependent inhibition of adenylyl cyclase to depress lipolysis in adipocytes or to link brain energy metabolism， cerebral blood flow and neuronal activity in brain tissue， the other by β-arrestin 2-coupled inhibition of NF-κB and NLRP3 to repress inflammation in macrophages. GPR81 dysfunction is closely related to obesity， dyslipidemia， insulin resistance， impaired glucose tolerance and type 2 diabetes. GPR81 dysfunction may be also involved in the occurrence and development of temporal lobe epilepsy， central fatigue and ischemic cerebrovascular disease. This article summarized the roles of lactate receptor GPR81 in lipid metabolism， inflammation and the central nervous system.