期刊
STEROIDS
卷 73, 期 9-10, 页码 985-991出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.steroids.2007.11.008
关键词
G-protein-coupled receptor; GABA(B) receptor; potassium channels; POMC neurons; GPR30
资金
- NIDDK NIH HHS [DK68098, R01 DK068098, R56 DK068098] Funding Source: Medline
- NINDS NIH HHS [R01 NS043330, R56 NS038809, NS43330, NS38809, R01 NS038809] Funding Source: Medline
Estrogens are involved in the hypothalamic control of multiple homeostatic functions including reproduction, stress responses, energy metabolism, sleep cycles, temperature regulation and motivated behaviors. The actions of 17 beta-estradiol (E(2)) in the brain have been attributed to the activation of estrogen receptors alpha and beta, as well as G-protein-coupled or other membrane-associated estrogen receptors. Recently, we have identified a putative membrane-associated estrogen receptor that is coupled to desensitization of GABA(B) receptors in guinea pig and mouse hypothalamic neurons including proopiomelanocortin (POMC) neurons. We have synthesized a new nonsteroidal compound, STX, which selectively targets the G alpha q-coupled phospholipase C-protein kinase C-protein kinase A pathway, and have established that STX is more potent than E(2) in mediating this desensitization in an ICI 182,780-sensitive manner in both guinea pig and mouse neurons. Both E(2) and STX are fully efficacious in estrogen receptor alpha, knock-out mice. Finally, we observed that the putative membrane-associated estrogen receptor is different from GPR30 in arcuate neurons using whole-cell patch recording in hypothalamic slices from GPR30 knock-out mice. Collectively, these findings suggest that the mER is distinct from ER alpha, ER beta or GPR30. Published by Elsevier Inc.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据