| Bioactivity | 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]. |
| Target | IC50: 1.025 μM (Acid-sensing ion channel 3 (ASIC-3)) |
| Invitro | 在急性分离的成年大鼠背根神经节 (DRG) 神经元中，A-317567 对所有 pH 4.5 诱发的 ASIC 电流产生浓度依赖性抑制，IC50 范围在 2 和 30 μM 之间。A-317567 等效地阻断类 ASIC3 电流的持续相，这是一种类似于克隆 ASIC3 的双相电流，在 DRG 中占主导地位[2] 。 |
| In Vivo | A-317567 (1-100 μmol/kg; i.p; once) 在 CFA 模型中具有完全镇痛作用 (ED50 of 17 μmol/kg)。在这些条件下，A-317567 对侧爪子的缩回潜伏期没有显着影响[2]。 Animal Model: |
| Name | A-317567 |
| CAS | 371217-32-2 |
| Formula | C27H31N3 |
| Molar Mass | 397.56 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 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. |