| Description |
A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM. A-317567 has antidepressant and antinociception effects[1][2].
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| Related Catalog |
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| Target |
IC50: 1.025 μM (Acid-sensing ion channel 3 (ASIC-3))[1]
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| In Vitro |
The effects of A-317567 on three distinct types of native ASIC currents evoked in acutely dissociated adult rat dorsal root ganglion (DRG) neurons are studied. A-317567 produces concentration-dependent inhibition of all pH 4.5-evoked ASIC currents with an IC50 ranging between 2 and 30 μM, depending upon the type of ASIC current activated. A-317567 equipotently blocks the sustained phase of ASIC3-like current, a biphasic current akin to cloned ASIC3, which is predominant in DRG[2].
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| In Vivo |
A-317567 is fully analgesic effects in the CFA model (ED50 of 17 μmol/kg, i.p., adult male Sprague-Dawley rats). There is no significant effect of A-317567 on the withdrawal latency of the contralateral paw under these conditions[2].
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| References |
[1]. Kuduk SD, et al. Synthesis, structure-activity relationship, and pharmacological profile of analogs of the ASIC-3 inhibitor A-317567. ACS Chem Neurosci. 2010 Jan 20;1(1):19-24. [2]. Dubé GR, et al. Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels. Pain. 2005 Sep;117(1-2):88-96.
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