Action of MK_7264 -Gefapixant- at human P2X3 and P2X2 and 3 receptors and in vivo efficacy in models of sensitisation
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D Richards, JR Gever, AP Ford, SJ Fountain

Biomedical Research Centre, School of Biological Sciences, University of East Anglia, Norwich, UK

British Journal of Pharmacology

The P2X3 receptor is an ATP_gated ion channel expressed by sensory afferent neurons and is used as a target to treat chronic sensitisation conditions. The first_in_class, selective P2X3 and P2X2/3 receptor antagonist, the diaminopyrimidine MK_7264 (gefapixant), has progressed to Phase III trials for refractory or unexplained chronic cough. We used patch clamp to elucidate the pharmacology and kinetics of MK_7264 and rat models of hypersensitivity and hyperalgesia to test its efficacy on these conditions.

BIOSEB Instruments Used:
Von Frey Filaments (Bio-VF-M)

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