| 名称 | CYM2503 |
| 描述 | 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). |
| 体外活性 | CYM2503 potentiated the galanin-stimulated IP1 accumulation in HEK293 cells stably expressing GalR2 receptor, whereas it exhibited no detectable affinity for the (125)I galanin-binding site of GalR2 receptor, an effect consistent with that of a positive allosteric modulator. |
| 体内活性 | In the rat Li-pilocarpine status epilepticus model, CYM2503, injected intraperitoneally, increased the latency to first electrographic seizure and the latency to first stage 3 behavioral seizure, decreased the latency to the establishment of status epilepticus, and dramatically decreased the mortality.?In a Li-pilocarpine seizure model in mice, CYM2503 increased the latency to first electrographic seizure and decreased the total time in seizure.?CYM2503 also attenuated electroshock-induced seizures in mice.?Thus, CYM2503 provides a starting point for the development of anticonvulsant therapy using the galanin R2 receptor as target. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 50 mg/mL (64.27 mM)
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| 关键字 | Neuropeptide Y Receptor | electrographic seizure | NPY receptor | CYM2503 | CYM-2503 | CYM 2503 | seizure | inhibit | Inhibitor | epilepsy | GalR2 |
| 相关产品 | AC-263093 | HT-2157 | Galanin (1-16), mouse, porcine, rat | L 152804 | GW438014A | Peptide YY (PYY) (3-36), human | Selvigaltin | SF-22 | JNJ-31020028 | DF-1012 FA | AR-M 1896 Acetate | AC-099 hydrochloride |
| 相关库 | 经典已知活性库 | 神经信号分子库 | 膜蛋白靶向化合物库 | 神经递质受体化合物库 | NO PAINS 化合物库 | 已知活性化合物库 | GPCR靶点分子库 |
United States
