Clinical data | |
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Other names | S1A; S1RA; MR-309 |
Identifiers | |
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CAS Number | |
ChemSpider | |
UNII | |
ChEMBL | |
Chemical and physical data | |
Formula | C20H23N3O2 |
Molar mass | 337.423 g·mol−1 |
3D model ( JSmol) | |
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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.
Clinical data | |
---|---|
Other names | S1A; S1RA; MR-309 |
Identifiers | |
| |
CAS Number | |
ChemSpider | |
UNII | |
ChEMBL | |
Chemical and physical data | |
Formula | C20H23N3O2 |
Molar mass | 337.423 g·mol−1 |
3D model ( JSmol) | |
| |
|
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.