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*
1Department of Mother and Child, University of Medicine and Pharmacy of Craiova, Romania
2Department of Pharmacology, School of Medicine, Temple University of Philadelphia, USA
3Research Centre of Gastroenterology and Hepatology, University of Medicine and Pharmacy of Craiova, Romania
4Gastroenterology Department, University of Medicine and Pharmacy of Craiova, Romania
5Neuroinflammation DPU GSK R&D, Shanghai, China
6Research Centre for Clinical and Experimental Medicine, University of Medicine and Pharmacy of Craiova, Romania
7Biochemistry Department, University of Medicine and Pharmacy of Craiova, Romania
8Biophysics Department, University of Medicine and Pharmacy of Craiova, Romania
9Biostatistics Department, University of Medicine and Pharmacy of Craiova, Romania
10Pharmacology Department, University of Medicine and Pharmacy of Craiova, Romania
*corresponding author: andrei.tica@umfcv.ro
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Abstract:
The “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.






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