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.
|Dosages||6, 20, and 60 mg/kg two times a day and continues up to a week|
|Administration||by intraplantar or oral|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO: 4 mg/mL (Need ultrasonic and adjust pH to 5-6 with HCl)|
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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Suramin sodium salt is a polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM).
|Clopidogrel hydrogen sulfate
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Clopidogrel (Plavix) is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease.
GW791343 hydrochloride is ahydrochloride salt form of GW791343, which is a non-competitive allosteric modulator of human P2X7 receptor inhibitor with pIC50 of 7.
Ticlopidine hydrochloride is a selective P2Y12 receptor antagonist.
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