Phosphocholine – an agonist of metabotropic but not of ionotropic functions of α9-containing nicotinic acetylcholine receptors

• DOI: 10.1038/srep28660
• Publication Date: 2016-06-28T09:18:55Z
• Authors: K. Richter; V. Mathes; M. Fronius; M. Althaus; A. Hecker; G. Krasteva-Christ; W. Padberg; A. J. Hone; J. M. McIntosh; A. Zakrzewicz; V. Grau
• Keywords: Phosphocholine; Homomeric

Abstract We demonstrated previously that phosphocholine and phosphocholine-modified macromolecules efficiently inhibit ATP-dependent release of interleukin-1β from human murine monocytes by a mechanism involving nicotinic acetylcholine receptors (nAChR). Interleukin-1β is potent pro-inflammatory cytokine innate immunity plays pivotal roles in host defence. Control vital as excessively high systemic levels cause life threatening inflammatory diseases. In spite its structural similarity to acetylcholine, there are no other reports on interactions with nAChR. this study, we demonstrate inhibits ion-channel function ATP receptor P2X7 monocytic cells via nAChR containing α9 α10 subunits. stark contrast choline, does not evoke ion current responses Xenopus laevis oocytes, which heterologously express functional homomeric composed subunits or heteromeric Preincubation these oocytes phosphocholine, however, attenuated choline-induced changes, suggesting may act silent agonist. conclude phophocholine activates immuno-modulatory expressed but stimulate canonical ionotropic functions.