Formulation: A solid
Formal Name: 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-benzenesulfonamide
Purity: ≥98%
Formula Markup: C14H19N5O4S
Formula Weight: 353,4
Shelf life (days): 1460
CAS Number: 1015787-98-0
Notes: Gefapixant is an allosteric antagonist of the purinergic P2X3 receptor.{51756} It inhibits agonist-induced P2X3 and P2X2/3 currents in 1321N1 cells co-expressing human P2X2 and P2X3 (IC50s = 153 and 220 nM, respectively) but does not inhibit P2X2 currents in the same cells at 10 µM. In vivo, gefapixant (30 mg/kg) increases the paw withdrawal threshold and decreases weight-bearing discomfort in a rat model of inflammatory hyperalgesia induced by complete Freund’s adjuvant (CFA) and a rat model of neuropathic pain induced by sciatic nerve injury. Gefapixant (10 mg/kg) improves cardiac function, reduces cardiac TNF-α levels, and prevents cardiac fibrosis in a rat model of myocardial infarction induced by left anterior descending (LAD) branch ligation.{51757} Formulations containing gefapixant have been used in the treatment of chronic cough.
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