Characterization of functional P2X(1) receptors in mouse megakaryocytes

Thrombosis Research
Masahiro Ikeda

Abstract

Although accumulating evidence within the past 5 years strongly supports the importance of platelet P2X(1) receptors in hemostasis and thrombosis, P2X(1) receptors of platelet and/or its progenitor cell, megakaryocyte, have not been fully characterized. The aim of this study was to electrophysiologically and pharmacologically characterize the functional P2X(1) receptors on mouse megakaryocytes. The currents in response to nucleotides were examined using the patch-clamp whole-cell recording. The agonist profile of megakaryocyte P2X(1) receptors was ATP>alpha,beta-methylene ATP>beta,gamma-methylene ATP. The P2X(1) receptors exhibited substantial monovalent as well as divalent cation permeability and the ratios of Na(+) to Cs(+) and Ca(2+) to Cs(+) permeability were 1 and 2.5, respectively. P2X receptor antagonists except suramin significantly inhibited the P2X(1) responses with an IC(50) values of 0.4 microM for pyridoxal-phosphate-6-azophenyl-2',4'-disulfonate (PPADS), 0.3 microM for 2',3'-O-(2,4,6-trinitophenyl)-adenosine 5'-triphosphate (TNP-ATP), 20 microM for reactive blue 2 (RB2), or 160 microM for 8,8'-(carbonylbis(imino-3,1-phenylene carbonylimino)bis(1,3,5-naphthalenetrisulfonic acid) (NF023), respectively. Suramin had n...Continue Reading

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Citations

Feb 20, 2008·The Journal of Experimental Medicine·Craig N MorrellCharles J Lowenstein
Sep 4, 2008·The Journal of Biological Chemistry·Joan A SimR Alan North
Oct 16, 2007·British Journal of Pharmacology·J A SimR A North
Aug 12, 2015·Purinergic Signalling·Geoffrey Burnstock
Jan 1, 2010·American Journal of Physiology. Cell Physiology·José P YoungAdam Myers

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