A-317491

A-317491

CAT N°: 19256
Price:

From 54.00 45.90

A-317491 is a non-nucleotide antagonist of the purinergic receptors P2X3 and P2X2/3 (Kis = 22-92 nM in a calcium influx assay) that is selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 µM).{39363} It reduces thermal hyperalgesia induced by complete Freund’s adjuvant in rats (ED50 = 30 µmol/kg, s.c.) and nociceptive responses to chemically-induced pain. Chronic administration of A-317491 (30 µmol/kg, twice daily) reduces early, but not late, phase pain in a mouse model of bone cancer.{39362} A-317491 does not readily cross the blood-brain barrier and reduces pain responses when applied topically in a rat model of inflammatory pain, indicating that it acts primarily at peripheral purinergic receptors.{39364}

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