| Bioactivity | SCS (Salicylidene salicylhydrazide) is a potent, allosteric and selective inhibitor of β1-containing GABAA receptors with an IC50 of 32 nM against α2β1γ1θ by VIPR measurement. SCS is also a chelator of metal ions[1]. |
| Target | IC50: 32 nM (α2β1γ1θ; by VIPR measurement)IC50: 4.5 nM (α2β1γ1θ), 5.3 nM (α2β1γ1), 7.9 nM (α1β1γ2s) (Measured by using whole-cell patch clamp) |
| Invitro | SCS (0.1 nM-3 μM) 对表达 α2β1γ1θ、α2β1γ1 和 α1β1γ2s 受体的 Ltk- 细胞的 GABA EC20 电流有浓度依赖性抑制作用，而对 α2β3γ2s 和 α1β2γ2s 受体无影响[1]。SCS 的抑制不依赖于电压或使用 (not voltage or use dependent)[1]。SCS 抑制 GABAA 受体所必需的结构决定因素位于 β1 亚基的精氨酸 238 和甘氨酸 335 区域。β1 亚基的 T255 和 I308 对于 SCS 的抑制是必需的[1]。 |
| In Vivo | SCS (Salicylidene salicylhydrazide; 500-1000 mg/kg, i.p. or 800-1000 mg/kg, oral) 使小鼠产生腹部收缩[2]。SCS (10-75 mg/kg; i.p.; once) 在小鼠中显示出抗强直性和阶段性疼痛和辣椒素痛觉的抗痛觉活性[2]。SCS (10-75 mg/kg; i.p.; once) 显示小鼠抗炎活性[2]。SCS (50 and 75 mg/kg; i.p.; once) 显示对神经性痛觉的抗痛觉活性[2]。 Animal Model: |
| Name | SCS |
| CAS | 3232-36-8 |
| Formula | C14H12N2O3 |
| Molar Mass | 256.26 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Thompson SA, et al. Salicylidene salicylhydrazide, a selective inhibitor of beta 1-containing GABAA receptors. Br J Pharmacol. 2004 May;142(1):97-106. [2]. Rukh L, et al. Efficacy assessment of salicylidene salicylhydrazide in chemotherapy associated peripheral neuropathy. Eur J Pharmacol. 2020 Dec 5;888:173481. |