| Identification | Back Directory | [Name]
Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) | [CAS]
2310299-91-1 | [Synonyms]
Gefapixant citrate
methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1) | [Molecular Formula]
C20H27N5O11S | [MOL File]
2310299-91-1.mol | [Molecular Weight]
545.52 |
| Chemical Properties | Back Directory | [form ]
Solid | [color ]
White to off-white | [InChIKey]
AIJVJYUOMCRFOE-UHFFFAOYSA-N | [SMILES]
C(O)(C(=O)O)(CC(=O)O)CC(=O)O.O(C1=CN=C(N)N=C1N)C1C=C(S(=O)(=O)N)C(OC)=CC=1C(C)C |
| Hazard Information | Back Directory | [Uses]
Gefapixant citrate is an orally active and potent purinergic P2X3 receptor (P2X3R) antagonist, with IC50 values of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. Gefapixant citrate can be used for the research of chronic cough and knee osteoarthritis[1][2][3]. | [in vivo]
Gefapixant citrate (7d bid, orally) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate)[2]. | [IC 50]
P2X3 Receptor | [References]
[1] Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267. DOI:10.3389/fncel.2013.00267
[2] Ford AP, In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26. DOI:10.1007/s11302-011-9271-6
[3] Martin Nguyen A, et al. Validation of a visual analog scale for assessing cough severity in patients with chronic cough. Ther Adv Respir Dis. 2021 Jan-Dec;15:17534666211049743. DOI:10.1177/17534666211049743 |
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