SPINORPHIN DERIVATIVES AS POTENT AND SELECTIVE HUMAN P2X3 RECEPTOR ANTAGONIST

摘要

The present invention relates to a spinorphin derivative useful as a potent and selective human P2X3 receptor antagonist. More particularly, the present invention provides a spinorphin derivative useful as a potent and selective human P2X3 receptor antagonist selected from peptide AVVYPWT, peptide LAVYPWT, peptide LVAYPWT, peptide LVVAPWT and/ or cyclic peptide LWYPWT. Human P2X3 receptor antagonist has been developed on the electrophysiological evaluation of spinorphin peptide derivatives, truncated peptide analogues, cyclic peptides and a retroinverso peptide at human P2X3 receptors to determine the channel blocking activity.