Romanian Society of Pharmaceutical Sciences

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CELL MEMBRANE GPER AND ERα ON MYOMETRIUM: TWO DISTINCT RECEPTORS WITH DISTINCT SIGNALLING PATHWAYS

OANA SORINA TICA1, ELENA DELIU2, TUDOREL CIUREA3,4, XIN GAO5, ANA-MARIA BUGA6,7, EUGEN OSIAC6,8, DRAGOS ALEXANDRU6,9, ANDREI ADRIAN TICA6,10*

1.Department of Mother and Child, University of Medicine and Pharmacy of Craiova, Romania
2.Department of Pharmacology, School of Medicine, Temple University of Philadelphia, USA
3.Research Centre of Gastroenterology and Hepatology, University of Medicine and Pharmacy of Craiova, Romania
4.Gastroenterology Department, University of Medicine and Pharmacy of Craiova, Romania
5.Neuroinflammation DPU GSK R&D, Shanghai, China
6.Research Centre for Clinical and Experimental Medicine, University of Medicine and Pharmacy of Craiova, Romania
7.Biochemistry Department, University of Medicine and Pharmacy of Craiova, Romania
8.Biophysics Department, University of Medicine and Pharmacy of Craiova, Romania
9.Biostatistics Department, University of Medicine and Pharmacy of Craiova, Romania
10.Pharmacology Department, University of Medicine and Pharmacy of Craiova, Romania

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he “rapid” effects of oestrogens on myometrium mainly result by activating cell membrane oestrogen receptors: ERα and GPER (G protein coupled oestrogen receptor 1). In contrast to the contractile effect induced by G-1 (GPER agonist), effect involving the opening of L-type calcium channels, oestradiol (E2) inhibited until arrest the spontaneous contractile activity and significantly decreased the contraction induced by high K+ or oxytocin. The effects of E2 were not blocked by G-15 (GPER antagonist). We concluded that the “rapid” effects E2-induced on myometrium are the result of cell membrane ERα activation and mainly consist of the inhibition of L-type calcium channels. It is a sticking difference between the genomic and non-genomic effect of E2 on oxytocin-induced signalling pathway. Finally, it is very probable a masking/inhibition (modulator) effect of ERα on cell membrane GPER activity.