Development & Structure-Activity Relationship Studies of Heterocyclic Compounds as Novel P2X3 Receptor Antagonists

Abstract

For the development of novel P2X3 receptor antagonists, I have synthesized heterocyclic derivatives and evaluated their activity through the fluo-4 Ca2+ influx assay. Through structure-activity relationship (SAR) studies, I have identified 6a as a potent P2X3 receptor antagonist with an IC50 value of 0.12 µM. The discovery of a novel P2X3 receptor antagonist, 6a, provides a valuable contribution to the field of new drug discovery programs targeting neuropathic pain.