[1]刘 磊,许婵娟,刘剑峰.GABAB受体变构调节剂及其应用研究进展[J].中国药理学通报,2018,(10):1352-1355.[doi:10.3969/j.issn.1001-1978.2018.10.006]
 LIU Lei,XU Chan-juan,LIU Jian-feng.Research progress of GABAB receptor allosteric modulators and their applications[J].Chinese Pharmacological Bulletin,2018,(10):1352-1355.[doi:10.3969/j.issn.1001-1978.2018.10.006]





Research progress of GABAB receptor allosteric modulators and their applications
刘 磊 许婵娟 刘剑峰
华中科技大学生命科学与技术学院,湖北 武汉 430074
LIU Lei XU Chan-juan LIU Jian-feng
College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074, China
GABAB受体 正位位点 正位配体 变构调节位点 变构调节剂 动物模型
GABAB receptor orthosteric site orthosteric ligand allosteric site allosteric modulator animal model
R-05; R392.11
GABAB receptor involves in the regulation of diverse physiological and pathological processes and has been one of the most important drug targets.Currently, drug development for the receptor mainly focuses on orthosteric ligands, and the marketed drugs are very limited.Allosteric modulators are novel ligands of the GABAB receptor, which specifically regulate receptor activity by acting on the allosteric modulatory sites and possess good receptor specificity and pharmacological characteristics.A variety of animal model experiments showed that GABAB receptor allosteric modulators could effectively improve the symptoms of various diseases, such as drug addiction and pain, by cooperating with orthosteric ligands, and exert novel characteristics other than orthosteric ligands.The unique physiological effects of GABAB receptor allosteric modulators set them as promising candidates, showing excellent medical application value and prospects.Further clinical trial verification and investigation of the detailed mechanism of allosteric modulators will provide new ideas for the development of new drugs.


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 SHAO Cai-feng,ZHANG Wen-wei,HU Chao-ting,et al.Effect of GABAB receptor agonist baclofen on excitatory and inhibitory synapses of ventrolateral periaqueductal gray in rats[J].Chinese Pharmacological Bulletin,2018,(10):1511.[doi:10.3969/j.issn.1001-1978.2018.11.008]


基金项目:国家自然科学基金资助项目(No 31711530146,31511130131,31301163)
作者简介:刘 磊(1986-),男,博士生,研究方向:GABAB受体变构调节,E-mail:lei_liu86@163.com;
更新日期/Last Update: 2018-08-26