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S1RA is a potent and selective sigma-1 receptor (σ1R, Ki=17 nM), which showes good selectivity against σ2R (Ki > 1000 nM). S1RA dose-dependently inhibites formalin-induced nociception (both phases), capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity.
| Molecular Weight | 337.42 |
| Formula | C20H23N3O2 |
| CAS Number | 878141-96-9 |
| Solubility (25°C) | DMSO 30 mg/mL (ultrasonic and warming and heat to 60°C) 1M HCl : 40 mg/mL (ultrasonic and adjust pH to 1 with HCl) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Sigma Receptor Products |
|---|
| Siramesine hydrochloride
Siramesine (Lu 28-179) hydrochloride is an effective sigma-2 receptor agonist. Siramesine has a nanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and is 140 times more selective for sigma-2 receptors (IC50=17 nM). Siramesine has xC-system inhibitory activity associated with iron death. |
| Siramesine
Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. |
| Pentoxyverine Citrate
Pentoxyverine citrate is an orally active sigma-1 receptor agonist with Ki values of 41 nM for σ1, 894 nM for σ2, and 75 nM for σ1 in guinea pig brain membranes.Pentoxyverine citrate is also a muscarinic antagonist. |
| Cutamesine dihydrochloride
Cutamesine dihydrochloride (SA4503 dihydrochloride; AGY94806 dihydrochloride) is a novel and selective opioid sigma1 receptor agonist with IC50 of 17.4 nM. |
| Veratramine
Veratramine (NSC17821; NSC23880) is a signal transduction inhibitor that acts on tumors. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities. |
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