S1RA (E-52862)是一种选择性sigma-1 receptor (σ1R)拮抗剂，对人源σ1受体的结合亲和力Ki为17 nM。 Information S1RA S1RA (E-52862) is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels. Targets σ1R 17 nM(Ki) In vitro S1RA behaves as a highly selective σ1 receptor antagonist. It shows high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). It has moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) against human 5-HT2B receptor. S1RA shows no significant affinity (Ki > 1 µM or % inhibition at 1 µM In vivo S1RA crosses the blood-brain barrier and binds to σ1 receptors in the CNS.
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S1RA
CAS number：878141-96-9 molecular formula：C20H23N3O2
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| Chinese alias | - | ||
| English alias | S1RA | 878141-96-9 | E-52862 | ZW18DSD1H4 | 4-(2-((5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yl)oxy)ethyl)morpholine | UNII-ZW18DSD1H4 | 4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine | CHEMBL2170062 | API-001 | 4-(2-(5-Methyl-1-(naphtha | ||
| CAS number | 878141-96-9 | molecular formula | C20H23N3O2 |
| molecular weight | 337.42 g/mol | Exact mass | - |
| PSA | 39.500 Ų | logp | 3.459 |
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