title: Functional expression of G protein-coupled receptor 30 in immature rat epididymal epithelium.
abstract: The aim of this study is to investigate the functional role of G protein-coupled receptor 30 (GPR30) in the epididymis. We found that GPR30 is expressed in the epithelium of the immature rat epididymis and is involved in chloride secretion into the caudal epididymis lumen. The short-circuit current (Isc) experiments showed that in primary cultured caudal epididymis epithelium, activation of GPR30 by its specific agonist G1 induced a mono-phasic current increase, and G15, the specific antagonist of GPR30, could completely inhibit the current induced by G1. The G1-induced Isc was largely blocked by application of the non-specific chloride channel inhibitor diphenylamine-dicarboxylic acid (DPC), or by the cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor CFTRinh-172, suggesting that the current was mainly mediated through CFTR. In addition, after stimulating GPR30 by G1, the intracellular concentration of cAMP in the epithelium was significantly increased, indicating that the cAMP signal pathway is involved and could be responsible for the CFTR activation. Finally, to further investigate the function of GPR30 in vivo, G15 was administrated into rats subcutaneously. The osmotic pressure of the micro perfusion solution from epididymis was measured and the sperms were collected. Results showed that there was an osmotic pressure increase of the perfusion solution from G15 treated rats. When the GPR30 was inhibited by G15 endogenously, the motility of sperms decreased. Our data demonstrated that GPR30 is involved in the formation of caudal epididymis fluid micro-environment thus affecting sperm motility.
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Xiaonian
authors.initials: X
authors.lastname: Cao
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Jiehong
authors.initials: J
authors.lastname: Huang
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Geng
authors.initials: G
authors.lastname: Zhang
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Wulin
authors.initials: W
authors.lastname: Zuo
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Chongfeng
authors.initials: C
authors.lastname: Lan
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Sun
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Dengliang
authors.initials: D
authors.lastname: Yang
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Dongdong
authors.initials: D
authors.lastname: Gao
authors.affiliation: School of Biomedical Sciences, the Chinese University of Hong Kong, Shatin, N.T., Hong Kong, China.
authors.forename: Christopher H K
authors.initials: CH
authors.lastname: Cheng
authors.affiliation: School of Life Sciences, Sun Yat-Sen University, Guangzhou, 510275, China.
authors.forename: Wen-Liang
authors.initials: WL
authors.lastname: Zhou
mesh_terms: D000818:Animals; D015153:Blotting, Western; D002478:Cells, Cultured; D002712:Chlorides / Q000378:metabolism; D000242:Cyclic AMP / Q000378:metabolism; D019005:Cystic Fibrosis Transmembrane Conductance Regulator / Q000037:antagonists & inhibitors / Q000378:metabolism; D004822:Epididymis / Q000166:cytology; D004847:Epithelial Cells / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D005786:Gene Expression Regulation / Q000187:drug effects; D008297:Male; D008856:Microscopy, Fluorescence; D009997:Osmotic Pressure / Q000187:drug effects; D018408:Patch-Clamp Techniques; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology; D015363:Quinolones / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D060888:Real-Time Polymerase Chain Reaction; D043562:Receptors, G-Protein-Coupled / Q000819:agonists / Q000037:antagonists & inhibitors / Q000235:genetics* / Q000378:metabolism; D013081:Sperm Motility / Q000187:drug effects
chemical_list: D002712:Chlorides; C520305:Gper1 protein, rat; D011804:Quinolines; D015363:Quinolones; D043562:Receptors, G-Protein-Coupled; D019005:Cystic Fibrosis Transmembrane Conductance Regulator; D000242:Cyclic AMP; C037219:quinoline
keywords: CFTR; GPR30; Isc; epididymis; sperm motility