| Name | A-317491 |
| Description | A-317491 (ABT 202) is a non-nucleotide P2X3 ( Ki: 22 nM) and P2X2/3 receptor (Ki: 9 nM) antagonist, which inhibits calcium flux mediated by the receptors. |
| In vitro | A-317491 blocks recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and is highly selective (IC50 >10 μM) over other P2 receptors and other ion channels, neurotransmitter receptors, and enzymes [1]. |
| In vivo | A-317491 dose-dependently reduces complete Freund's adjuvant-induced thermal hyperalgesia in the rat (ED50: 30 μmol/kg s.c.). A-317491 is most potent in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury (ED50: 10-15 μmol/kg s.c.). Although active in chronic pain models, A-317491 is ineffective in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain (ED50 >100 μmol/kg s.c.) [1]. A-317491 is effective in reducing pain associated behavior in several animal models of inflammatory and neuropathic pain when administered systemically [2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 47 mg/mL (83.1 mM), Sonication is recommended.
Ethanol : 90 mg/mL (159.13 mM), Sonication is recommended.
H2O : < 0.1 mg/mL (insoluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.54 mM), Sonication is recommended.
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| Keywords | pain | P2XRs | P2XReceptor | P2X3 | P2X2/3 | P2X2 | P2X Receptor | neuropathic | Inhibitor | inhibit | inflammatory | Human P2X3 | flux | calcium | ABT-202 | ABT202 | A-317491 | A317491 | A 317491 |
| Inhibitors Related | Gefapixant citrate | Eperisone hydrochloride | Aurintricarboxylic acid | Sodium metatungstate | NP-1815-PX | (E/Z)-Sivopixant | PSB-12062 | ATP disodium salt | Oxatomide | Ivermectin | Lappaconitine | Paroxetine |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Neurotransmitter Receptor Compound Library | Multi-Target Compound Library | Inhibitor Library | NO PAINS Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
