| 1 | GPR3,GPR6,and GPR12 as novel molecular targets:their biological functions and interaction with cannabidiol显示文摘The G protein-coupled receptors 3,6,and 12(GPR3,GPR6,and GPR12)comprise a family of closely related orphan receptors with no con firmed en dogenous liga nds.These receptors are con stitutively active and capable of signaling through G protein-mediated and non-G protein-mediated mechanisms.These orphan receptors have previously been reported to play important roles in many normal physiological functions and to be involved in a variety of pathological conditions.Although they are orphans,GPR3,GPR6,and GPR12 are phylogenetically most closely related to the cannabinoid receptors.Using β-arrestin2 recruitment and cAMP accumulati on assays,we recently found that the non psychoactive phytoca nnabinoid cann abidiol(CBD)is an inverse agonist for GPR3,GPR6,and GPR12.This discovery highlights these orphan receptors as potential new molecular targets for CBD,provides novel mechanisms of action,and suggests new therapeutic uses of CBD for illnesses such as Alzheimer's disease,Parkinson's disease,can cer,and infertility.Furthermore,identificati on of CBD as a new in verse agonist for GPR3,GPR6,and GPR12 provides the initial chemical scaffolds upon which potent and efficacious agents acting on these receptors can be developed,with the goal of developing chemical tools for studying these orphan receptors and ultimately new therapeutic agents. | Alyssa S.Laun Sarah H.Shrader Kevin J.Brown Zhao-Hui Song | 2019 | Acta Pharmacologica Sinica2019，40，3： | 2 |
您所在的机构暂未开通此部分的功能，请联系管理员