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- Title
Non-genomic inhibition of human P2X<sub>7</sub> purinoceptor by 17β-oestradiol.
- Authors
Cario-Toumaniantz, Chrystelle; Loirand, Gervaise; Ferrier, Laurent; Pacaud, Pierre
- Abstract
Effects of oestrogen on the current evoked by ATP and benzoylbenzoyl ATP (BzATP) in CV-1 monkey kidney cells transformed by SV 40 (COS cells) expressing the human P2X7 (hP2X7) purinoceptor were studied using standard patch-clamp techniques., 17β-Oestradiol rapidly and reversibly inhibited the whole-cell hP2X7 receptor cation current. This inhibitory action resulted in a rightward shift of the dose-response curve to ATP and BzATP in the presence of physiological as well as low divalent cation concentrations., The inhibitory effect of 17β-oestradiol on the BzATP- or ATP-induced cation current was concentration dependent. The half-maximal inhibition was obtained with 3 μM 17β-oestradiol. Progesterone and 17α-oestradiol had almost no effect on the hP2X7 receptor cation current., The inhibition of the hP2X7 receptor cation current by 17β-oestradiol did not depend on the membrane potential. 17β-Oestradiol added to the extracellular side of outside-out patches inhibited BzATP-activated single-channel currents., Activation of the hP2X7 receptor in both COS and U937 (human macrophage) cells did not induce the formation of large non-specific pores., Since COS cells do not express endogenous nuclear oestrogen receptor, this study shows that, at pharmacological concentrations, 17β-oestradiol inhibited the hP2X7 receptor cation channel in a non-genomic manner.
- Publication
Journal of Physiology, 1998, Vol 508, Issue 3, p659
- ISSN
0022-3751
- Publication type
Article
- DOI
10.1111/j.1469-7793.1998.659bp.x