Sigma-1 receptor antagonist 7
Sigma-1 receptor antagonist 7 is a selective sigma-1 receptor antagonist capable of crossing the blood-brain barrier, with an IC50 of 12.7 nM against guinea pig σ1R. Sigma-1 receptor antagonist 7 binds to σ1R, and its binding affinity decreases in the presence of Phenytoin (HY-B0448). Sigma-1 receptor antagonist 7 alleviates mechanical and thermal hyperalgesia induced by acute inflammation in rats. Sigma-1 receptor antagonist 7 can be used for research related to hyperalgesia.
For research use only. We do not sell to patients.
- CAS No.: 3050643-44-9
- Formula: C22H32N2O
- Molecular Weight:340.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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Sigma 1 Receptor 12.7 nM (IC50) |
Sigma-1 receptor antagonist 7 (compound 52) (135 min) potently binds to guinea pig brain-derived Sigma-1 receptor with a Ki of 8.6 nM and an IC50 of 12.7 nM[1].
Sigma-1 receptor antagonist 7 (135 min) shows weak binding to guinea pig-derived sigma-2 receptors with an IC50 of 1275.1 nM, demonstrating ~100-fold selectivity for sigma-1 receptors[1].
Sigma-1 receptor antagonist 7 (135 min) acts as a sigma-1 receptor antagonist, as evidenced by its increased Ki value (from 13.2 nM to 47.1 nM) in the presence of 1 mM phenytoin in guinea pig brain membrane assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCINF_obs | Brain Concentration | Plasma Concentration |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.p. | 2.79 h | 0.37 h | 2269 ng/mL | 4536.34 ng·h/mL | 4538.46 ng·h/mL | 5503 ng/mL | 1430 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 8-week-old, 200-300 g, intraplantar injection of 100 μL 1% w/v λ-carrageenan to induce inflammatory hyperalgesia)[1]
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Dosage:10 mg/kg; 20 mg/kg; 30 mg/kg; 40 mg/kg
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Administration:i.p.; single dose
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Result:Prolonged the withdrawal latency of the inflamed paw in a dose-dependent manner, with an ED50 value of 23.0 mg/kg.
Significantly decreased the Δ latency (difference in withdrawal latency between inflamed and contralateral paws) at doses of 30 mg/kg and above.
Increased the withdrawal threshold of the inflamed paw in a dose-dependent manner, with an ED50 value of 19.4 mg/kg.
Significantly decreased the Δ threshold (difference in withdrawal threshold between inflamed and contralateral paws) at doses of 30 mg/kg and above.
Showed similar antihyperalgesic effects to the clinical candidate E52862 at 30 mg/kg.
Had its antihyperalgesic effect on withdrawal latency and Δ latency abolished by pretreatment with σ1R agonist PRE-084 (40 mg/kg).
Had its antihyperalgesic effect on withdrawal threshold and Δ threshold abolished by pretreatment with σ1R agonist PRE-084 (40 mg/kg).
Chemical Information
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CAS No. 3050643-44-9
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Molecular Weight 340.50
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Formula C22H32N2O
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SMILES
O=C1N(CC2CCCC2)CC3(CCN(CCC4=CC=CC=C4)CC3)C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Sigma-1 receptor antagonist 7 Related Classifications
HY-187185 Related Classifications
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