Chemistry:E-52862
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| Other names | S1A; S1RA; MR-309 |
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| Formula | C20H23N3O2 |
| Molar mass | 337.423 g·mol−1 |
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E-52862, also known as sigma-1 receptor antagonist (S1A, S1RA), as well as MR-309, 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.[1][2] 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.[2][3][4][5]
S1RA is being developed by Esteve for the treatment of neuropathic pain and the potentiation of opioid analgesia and has successfully completed Phase I clinical trials showing good safety and tolerability, and a pharmacokinetic profile compatible with once a day oral administration.[6] Phase II clinical trials are currently underway, making S1RA the first selective sigma-1 receptor antagonist evaluated in humans for these conditions.
See also
References
- ↑ "Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)". J. Med. Chem. 55 (19): 8211–8224. 2012. doi:10.1021/jm3007323. PMID 22784008.
- ↑ 2.0 2.1 "Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization". Br. J. Pharmacol. 166 (8): 2289–2306. 2012. doi:10.1111/j.1476-5381.2012.01942.x. PMID 22404321.
- ↑ "Role of sigma-1 receptors in paclitaxel-induced neuropathic pain in mice". J. Pain 13 (11): 1107–1121. 2012. doi:10.1016/j.jpain.2012.08.006. PMID 23063344.
- ↑ "Operant self-administration of a sigma ligand improves nociceptive and emotional manifestations of neuropathic pain". Eur. J. Pain 17 (6): 832–843. 2013. doi:10.1002/j.1532-2149.2012.00251.x. PMID 23172791.
- ↑ "σ1 receptors are involved in the visceral pain induced by intracolonic administration of capsaicin in Mice". Anesthesiology 118 (3): 691–700. 2013. doi:10.1097/ALN.0b013e318280a60a. PMID 23299362.
- ↑ "Safety, tolerability and pharmacokinetics of single and multiple doses of a novel sigma-1 receptor antagonist in three randomized phase I studies". Br. J. Clin. Pharmacol. 75 (1): 103–117. 2013. doi:10.1111/j.1365-2125.2012.04333.x. PMID 22607269.
External links
- [1] (Compound datasheet in Esteve company website)
- E-52862 - AdisInsight
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