A P2X3 and P2X2/3 receptor antagonist (Kis = 22-92 nM in a calcium influx assay); selective over other purinergic and neurotransmitter receptors

A-317491 – 25 mg

Brand:
Cayman
CAS:
475205-49-3
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A P2X3 and P2X2/3 receptor antagonist (Kis = 22-92 nM in a calcium influx assay); selective over other purinergic and neurotransmitter receptors, ion channels, and enzymes (IC50s = >10 µM); 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 reduces early, but not late, phase pain in a mouse model of bone cancer; does not readily cross the blood-brain barrier and reduces pain responses when applied topically,

Formal name: 5-[[[(3-phenoxyphenyl)methyl][(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]carbonyl]-1,2,4-benzenetricarboxylic acid

Synonyms: 

Molecular weight: 565.6

CAS: 475205-49-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation||Research Area|Neuroscience|Pain Research

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