AF-353 (hydrochloride) |
| Katalog-Nr.GC52495 |
A dual P2X3 and P2X2/3 receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 927887-18-1
Sample solution is provided at 25 µL, 10mM.
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AF-353 is a noncompetitive dual antagonist of the purinoreceptors P2X3 and P2X2/3 (IC50s = 10 and 79.4 nM, respectively).1,2 It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 (IC50 = >10 µM for all).2 It inhibits calcium flux in CHO-K1 cells expressing the rat P2X3 receptor and in 1321N1 cells expressing the human P2X3 and P2X2/3 receptors (IC50s = 8.91, 8.71, and 38.9 nM, respectively). AF-353 decreases the electrical signals in the detrusor, but not striated, muscle of the bladder in female rats.3
1.Carter, D.S., Alam, M., Cai, H., et al.Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X3/P2X2/3 antagonist for the treatment of painBioorg. Med. Chem. Lett.19(6)1628-1631(2009) 2.Gever, J.R., Soto, R., Henningsen, R.A., et al.AF-353, a novel, potent and orally bioavailable P2X3/P2X2/3 receptor antagonistBr. J. Pharmacol.160(6)1387-1398(2010) 3.Salazar, B.H., Hoffman, K.A., Zhang, C., et al.Electrical activity of the bladder Is attenuated by intravesical inhibition of P2X2/3 receptors during micturition in female ratsInt. Neurourol. J.21(4)259-269(2017)
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