Sigma-1 receptor antagonist 4_product_DataBase

Bioactivity	Sigma-1 receptor antagonist 4 (Compound 32) is a potent σ1R antagonist that significantly enhances the analgesic effect of morphine and rescues morphine-induced analgesic tolerance, with therapeutic potential to prevent morphine tolerance[1].
Target	IC50: 19.1 ± 0.6 nM (σ1R)
In Vivo	Sigma-1 receptor antagonist 4（0–60 mg/kg；腹腔注射；单次剂量）在 40 mg/kg 剂量范围内以剂量依赖性方式增强吗啡诱导的镇痛作用[1]。Sigma-1 receptor antagonist 4（30 mg/kg；腹腔注射；单剂量）通过增强吗啡诱导的 MOR 激动作用来增强抗伤害作用[1]。 Animal Model:
Name	Sigma-1 receptor antagonist 4
Formula	C22H26N2O
Molar Mass	334.45
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Fu K, et al. 2,6-diazaspiro[3.4]octan-7-one derivatives as potent sigma-1 receptor antagonists that enhanced the antinociceptive effect of morphine and rescued morphine tolerance. Eur J Med Chem. 2023 Mar 5;249:115178.

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