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The aim of our study was to determine the role of activation of classical estrogen receptors (ER) and novel membrane receptor, G protein\u2010coupled estrogen receptor (<jats:styled-content style=\"fixed-case\">GPER<\/jats:styled-content>) in human and mouse tissue and to assess the possible cross talk between these receptors in the <jats:styled-content style=\"fixed-case\">GI<\/jats:styled-content> tract.<\/jats:p><\/jats:sec><jats:sec><jats:title>Methods<\/jats:title><jats:p>Immunohistochemistry was used to determine the expression of <jats:styled-content style=\"fixed-case\">GPER<\/jats:styled-content> in human and mouse intestines. The effect of G\u20101, a <jats:styled-content style=\"fixed-case\">GPER<\/jats:styled-content> selective agonist, and estradiol, a non\u2010selective <jats:styled-content style=\"fixed-case\">ER<\/jats:styled-content> agonist, on muscle contractility was characterized in isolated preparations of the human and mouse colon. To characterize the effect of G\u20101 and estradiol <jats:italic>in vivo<\/jats:italic>, colonic bead expulsion test was performed. G\u20101 and estradiol activity on the visceral pain signaling was assessed in the mustard oil\u2010induced abdominal pain model.<\/jats:p><\/jats:sec><jats:sec><jats:title>Key Results<\/jats:title><jats:p>GPER is expressed in the human colon and in the mouse colon and ileum. G\u20101 and estradiol inhibited muscle contractility <jats:italic>in vitro<\/jats:italic> in human and mouse colon. G\u20101 or estradiol administered intravenously at the dose of 20\u00a0mg\/kg significantly prolonged the time to bead expulsion in females. Moreover, G\u20101 prolonged the time to bead expulsion and inhibited <jats:styled-content style=\"fixed-case\">GI<\/jats:styled-content> hypermotility in both genders. The injection of G\u20101 or estradiol resulted in a significant reduction in the number of pain\u2010induced behaviors in mice.<\/jats:p><\/jats:sec><jats:sec><jats:title>Conclusions and Inferences<\/jats:title><jats:p>GPER and <jats:styled-content style=\"fixed-case\">ER<\/jats:styled-content> receptors are involved in the regulation of <jats:styled-content style=\"fixed-case\">GI<\/jats:styled-content> motility and visceral pain. Both may thus constitute an important pharmacological target in the <jats:styled-content style=\"fixed-case\">IBS<\/jats:styled-content>\u2010D therapy.<\/jats:p><\/jats:sec>","DOI":"10.1111\/nmo.13025","type":"journal-article","created":{"date-parts":[[2017,2,13]],"date-time":"2017-02-13T04:42:38Z","timestamp":1486960958000},"source":"Crossref","is-referenced-by-count":67,"title":["G protein\u2010coupled estrogen receptor and estrogen receptor ligands regulate colonic motility and visceral pain"],"prefix":"10.1111","volume":"29","author":[{"given":"M.","family":"Zieli\u0144ska","sequence":"first","affiliation":[{"name":"Department of Biochemistry Faculty of Medicine Medical University of Lodz Lodz Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"J.","family":"Fichna","sequence":"additional","affiliation":[{"name":"Department of Biochemistry Faculty of Medicine Medical University of Lodz Lodz Poland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M.","family":"Bashashati","sequence":"additional","affiliation":[{"name":"Division of Gastroenterology Department of Internal Medicine Texas Tech University Health Sciences Center\/Paul L. 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