{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,30]],"date-time":"2026-09-30T11:13:22Z","timestamp":1790766802970,"version":"4.1.0"},"reference-count":50,"publisher":"American Physiological Society","issue":"5","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["American Journal of Physiology-Cell Physiology"],"published-print":{"date-parts":[[2011,11]]},"abstract":"<jats:p> G protein-coupled estrogen receptor 1 (GPER), also named GPR30, has been previously identified in the female reproductive system. In this study, GPER expression was found in the female rat myometrium by reverse transcriptase-polymerase chain reaction and immunocytochemistry. Using GPER-selective ligands, we assessed the effects of the GPER activation on resting membrane potential and cytosolic Ca<jats:sup>2+<\/jats:sup> concentration ([Ca<jats:sup>2+<\/jats:sup>]<jats:sub>i<\/jats:sub>) in rat myometrial cells, as well as on contractility of rat uterine strips. G-1, a specific GPER agonist, induced a concentration-dependent depolarization and increase in [Ca<jats:sup>2+<\/jats:sup>]<jats:sub>i<\/jats:sub> in myometrial cells. The depolarization was abolished in Na<jats:sup>+<\/jats:sup>-free saline. G-1-induced [Ca<jats:sup>2+<\/jats:sup>]<jats:sub>i<\/jats:sub> increase was markedly decreased by nifedipine, a L-type Ca<jats:sup>2+<\/jats:sup> channel blocker, by Ca<jats:sup>2+<\/jats:sup>-free or Na<jats:sup>+<\/jats:sup>-free saline. Intracellular administration of G-1 produced a faster and transitory increase in [Ca<jats:sup>2+<\/jats:sup>]<jats:sub>i<\/jats:sub>, with a higher amplitude than that induced by extracellular application, supporting an intracellular localization of the functional GPER in myometrial cells. Depletion of internal Ca<jats:sup>2+<\/jats:sup> stores with thapsigargin produced a robust store-activated Ca<jats:sup>2+<\/jats:sup> entry; the Ca<jats:sup>2+<\/jats:sup> response to G-1 was similar to the constitutive Ca<jats:sup>2+<\/jats:sup> entry and did not seem to involve store-operated Ca<jats:sup>2+<\/jats:sup> entry. In rat uterine strips, administration of G-1 increased the frequency and amplitude of contractions and the area under the contractility curve. The effects of G-1 on membrane potential, [Ca<jats:sup>2+<\/jats:sup>]<jats:sub>i<\/jats:sub>, and uterine contractility were prevented by pretreatment with G-15, a GPER antagonist, further supporting the involvement of GPER in these responses. Taken together, our results indicate that GPER is expressed and functional in rat myometrium. GPER activation produces depolarization, elevates [Ca<jats:sup>2+<\/jats:sup>]<jats:sub>i<\/jats:sub> and increases contractility in myometrial cells. <\/jats:p>","DOI":"10.1152\/ajpcell.00501.2010","type":"journal-article","created":{"date-parts":[[2011,8,25]],"date-time":"2011-08-25T04:31:25Z","timestamp":1314246685000},"page":"C1262-C1269","source":"Crossref","is-referenced-by-count":36,"title":["G protein-coupled estrogen receptor 1-mediated effects in the rat myometrium"],"prefix":"10.1152","volume":"301","author":[{"given":"Andrei A.","family":"Tica","sequence":"first","affiliation":[{"name":"Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Erica C.","family":"Dun","sequence":"additional","affiliation":[{"name":"Department of Gynecology and Obstetrics, Emory University School of Medicine, Atlanta, Georgia;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Oana S.","family":"Tica","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xin","family":"Gao","sequence":"additional","affiliation":[{"name":"Department of Pharmacology, Temple University School of Medicine, Philadelphia, Pennsylvania;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jeffrey B.","family":"Arterburn","sequence":"additional","affiliation":[{"name":"Department of Chemistry and Biochemistry, New Mexico State University, Las Cruces;"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"G. 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