For research use only. Not for therapeutic Use.
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].
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 μM. 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 μmol/kg; i.p; once) is fully analgesic effects in the CFA model (ED50 of 17 μmol/kg). There is no significant effect of A-317567 on the withdrawal latency of the contralateral paw under these conditions[2].
| Catalog Number | I000209 |
| CAS Number | 371217-32-2 |
| Synonyms | 6-[2-(2-methyl-1-propan-2-yl-3,4-dihydro-1H-isoquinolin-7-yl)cyclopropyl]naphthalene-2-carboximidamide |
| Molecular Formula | C27H31N3 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H31N3/c1-16(2)26-25-14-21(7-4-17(25)10-11-30(26)3)24-15-23(24)20-8-5-19-13-22(27(28)29)9-6-18(19)12-20/h4-9,12-14,16,23-24,26H,10-11,15H2,1-3H3,(H3,28,29) |
| InChIKey | FEPIUXBUJVISNN-UHFFFAOYSA-N |
| SMILES | CC(C)C1C2=C(CCN1C)C=CC(=C2)C3CC3C4=CC5=C(C=C4)C=C(C=C5)C(=N)N |
| Reference | [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. |
