| Description | CYM2503 is a positive allosteric modulator (PAM) of the GAL2 receptor that potentiates galanin-induced IP1 production in vitro. It has no affinity for the orthosteric galanin binding site of the receptor (as measured by its inability to displace iodinated galanin, or to induce IP1 accumulation on its own). |
| In vitro | CYM2503在稳定表达GalR2受体的HEK293细胞中增强了galanin刺激下的IP1累积，但对GalR2受体的(125)I galanin结合位点没有检测到明显亲和力，这一效应与阳性变构调节剂一致。 |
| In vivo | 在大鼠Li-pilocarpine状态性癫痫模型中，通过腹腔注射CYM2503能够增加首次电图性 seizure 的潜伏期和第一阶段行为性 seizure 的潜伏期，减少状态性癫痫建立的潜伏期，并显著降低死亡率。在小鼠Li-pilocarpine seizure 模型中，CYM2503增加了首次电图性 seizure 的潜伏期，减少了 seizure 总时间。CYM2503还能减轻小鼠电击诱发的 seizures。因此，CYM2503为使用 galanin R2 受体作为靶点开发抗癫痫治疗提供了一个起点。 |
| molecular weight | 777.95 |
| Molecular formula | C45H55N5O7 |
| CAS | 1308833-36-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (64.27 mM) |
| References | 1. Lu X , Roberts R , Xia R , et al. GalR2-positive allosteric modulator exhibits anticonvulsant effects in animal models[J]. Proc Natl Acad Sci U S A, 2010, 107(34):15229-15234. |