Gefapixant (AF-219) is an orally active small molecule antagonist at human P2X3-containing receptors, with IC50s of ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
In vivo, in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate), Gefapixant (7d bid, orally; right) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses.
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Concentrations | |
Incubation time |
Animal Experiment | |
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Animal models | Rats |
Formulation | |
Dosages | 6, 20, and 60 mg/kg two times a day and continues up to a week |
Administration | by intraplantar or oral |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Molecular Weight | 353.40 |
Formula | C14H19N5O4S |
CAS Number | 1015787-98-0 |
Purity | >98% |
Solubility | DMSO: 4 mg/mL (Need ultrasonic and adjust pH to 5-6 with HCl) |
Storage | at -20°C |
P2X3 receptor antagonist (AF-219) in refractory chronic cough: a randomised, double-blind, placebo-controlled phase 2 study.
Abdulqawi R, et al. Lancet. 2015 Mar 28;385(9974):1198-205. PMID: 25467586.
The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders.
Ford AP, et al. Front Cell Neurosci. 2013 Dec 19;7:267. PMID: 24391544.
In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization.
Ford AP, et al. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26. PMID: 22095157.
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