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Selective potentiation of homomeric P2X2 ionotropic ATP receptors by a fast non-genomic action of progesterone.
Neuropharmacology 2010; 58(3):569-77N

Abstract

P2X receptors are ligand-gated ion channels activated by ATP that are widely expressed in the organism and regulate many physiological functions. We have studied the effect of progesterone (PROG) on native P2X receptors present in rat dorsal root ganglion (DRG) neurons and on recombinant P2X receptors expressed in HEK293 cells or Xenopus laevis oocytes. The effects of PROG were observed and already maximal during the first coapplication with ATP and did not need any preincubation of the cells with PROG, indicating a fast mechanism of action. In DRG neurons, PROG rapidly and reversibly potentiated submaximal but not saturating plateau-like currents evoked by ATP, but had no effect on the currents activated by alpha,beta-methylene ATP, an agonist of homomeric or heteromeric receptors containing P2X1 or P2X3 subunits. In cells expressing homomeric P2X2 receptors, responses to submaximal ATP, were systematically potentiated by PROG in a dose-dependent manner with a threshold between 1 and 10 nM. PROG had no effect on ATP currents carried by homomeric P2X1, P2X3, and P2X4 receptors or by heteromeric P2X1/5 and P2X2/3 receptors. We conclude that PROG selectively potentiates homomeric P2X2 receptors and, in contrast with dehydroepiandrosterone (DHEA), discriminates between homomeric and heteromeric P2X2-containing receptors. This might have important physiological implications since the P2X2 subunit is the most widely distributed P2X subunit in the organism. Moreover, DHEA and PROG might be useful tools to clarify the distribution and the role of native homo- and heteromeric P2X2 receptors.

Authors+Show Affiliations

Institut des Neurosciences Cellulaires et Intégratives, UPR 3212 Centre National de la Recherche Scientifique, Université de Strasbourg, Département Nociception et Douleur, 21 rue René Descartes, F-67084 Strasbourg cedex, France.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20004677

Citation

De Roo, Mathias, et al. "Selective Potentiation of Homomeric P2X2 Ionotropic ATP Receptors By a Fast Non-genomic Action of Progesterone." Neuropharmacology, vol. 58, no. 3, 2010, pp. 569-77.
De Roo M, Boué-Grabot E, Schlichter R. Selective potentiation of homomeric P2X2 ionotropic ATP receptors by a fast non-genomic action of progesterone. Neuropharmacology. 2010;58(3):569-77.
De Roo, M., Boué-Grabot, E., & Schlichter, R. (2010). Selective potentiation of homomeric P2X2 ionotropic ATP receptors by a fast non-genomic action of progesterone. Neuropharmacology, 58(3), pp. 569-77. doi:10.1016/j.neuropharm.2009.12.002.
De Roo M, Boué-Grabot E, Schlichter R. Selective Potentiation of Homomeric P2X2 Ionotropic ATP Receptors By a Fast Non-genomic Action of Progesterone. Neuropharmacology. 2010;58(3):569-77. PubMed PMID: 20004677.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Selective potentiation of homomeric P2X2 ionotropic ATP receptors by a fast non-genomic action of progesterone. AU - De Roo,Mathias, AU - Boué-Grabot,Eric, AU - Schlichter,Rémy, Y1 - 2009/12/16/ PY - 2009/04/08/received PY - 2009/11/06/revised PY - 2009/12/02/accepted PY - 2009/12/17/entrez PY - 2009/12/17/pubmed PY - 2010/4/8/medline SP - 569 EP - 77 JF - Neuropharmacology JO - Neuropharmacology VL - 58 IS - 3 N2 - P2X receptors are ligand-gated ion channels activated by ATP that are widely expressed in the organism and regulate many physiological functions. We have studied the effect of progesterone (PROG) on native P2X receptors present in rat dorsal root ganglion (DRG) neurons and on recombinant P2X receptors expressed in HEK293 cells or Xenopus laevis oocytes. The effects of PROG were observed and already maximal during the first coapplication with ATP and did not need any preincubation of the cells with PROG, indicating a fast mechanism of action. In DRG neurons, PROG rapidly and reversibly potentiated submaximal but not saturating plateau-like currents evoked by ATP, but had no effect on the currents activated by alpha,beta-methylene ATP, an agonist of homomeric or heteromeric receptors containing P2X1 or P2X3 subunits. In cells expressing homomeric P2X2 receptors, responses to submaximal ATP, were systematically potentiated by PROG in a dose-dependent manner with a threshold between 1 and 10 nM. PROG had no effect on ATP currents carried by homomeric P2X1, P2X3, and P2X4 receptors or by heteromeric P2X1/5 and P2X2/3 receptors. We conclude that PROG selectively potentiates homomeric P2X2 receptors and, in contrast with dehydroepiandrosterone (DHEA), discriminates between homomeric and heteromeric P2X2-containing receptors. This might have important physiological implications since the P2X2 subunit is the most widely distributed P2X subunit in the organism. Moreover, DHEA and PROG might be useful tools to clarify the distribution and the role of native homo- and heteromeric P2X2 receptors. SN - 1873-7064 UR - https://www.unboundmedicine.com/medline/citation/20004677/Selective_potentiation_of_homomeric_P2X2_ionotropic_ATP_receptors_by_a_fast_non_genomic_action_of_progesterone_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0028-3908(09)00368-2 DB - PRIME DP - Unbound Medicine ER -