S1RA hydrochloride
| CAS号 | 1265917-14-3 | 货号 | BCP24076 |
| 中文名 | S1RA hydrochloride | ||
| 英文名 | S1RA hydrochloride | ||
| 中文别名 | |||
| 英文别名 | E52862 HCl;E-52862 hydrochloride;; E-52862 HCl; E 52862 hydrochloride; S1RA hydrochloride; | ||
| 分子式 | C20H24ClN3O2 | 分子量 | 373.88 |
| 生物活性 | S1RA Hcl(E-52862 Hcl) is a potent and selective sigma-1 receptor(σ1R, Ki=17 nM) antagonist, showed good selectivity against σ2R (Ki > 1000 nM).E-52862, also known as S1RA, is a selective sigma-1 receptor antagonist, with a reported binding affinity of Ki = 17.0 ± 7.0 nM, selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. In preclinical studies, S1RA has demonstrated efficacy in relieving neuropathic pain and pain in other sensitizing conditions, associated with an improvement of the emotional negative state. E-52862 attenuates neuropathic pain of different aetiology in rats. | ||
| 信号通路 | GPCR/G Protein | ||
| 靶 点 | Sigma Receptor | ||
结构式
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