In acutely dissociated adult rat dorsal root ganglion (DRG) neurons, A-317567 produces concentration-dependent inhibition of all pH 4.5-evoked ASIC currents with an IC50 ranging between 2 and 30 渭M. A-317567 equipotently blocks the sustained phase of ASIC3-like current, a biphasic current akin to cloned ASIC3, which is predominant in DRG[2].
A-317567 (1-100 渭mol/kg; i.p; once) is fully analgesic effects in the CFA model (ED50 of 17 渭mol/kg). There is no significant effect of A-317567 on the withdrawal latency of the contralateral paw under these conditions[2].
[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]. Dub茅 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.