Cutamesine  (Synonyms: SA4503; AGY 94806)

Cutamesine (SA4503) is a potent and selective sigma 1 receptor agonist with an IC₅₀ of 17.4 nM in guinea pig brain membranes. Cutamesine shows >100-fold less affinity for the sigma 2 receptor (IC₅₀ of 1784 nM). Cutamesine has antidepressant effects^[1][2].

将神经元暴露于 H₂O₂ 会导致细胞死亡，而用 Cutamesine 预处理可抑制神经元细胞死亡。Cutamesine 还能降低 MAPK/ERK 通路的激活，并下调离子型谷氨酸受体 GluR1^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

在麻醉雄性 Sprague-Dawley 大鼠的黑质致密部 (SNC) 和腹侧被盖区 (VTA) 中，Cutamesine (0.01-1.28 mg/kg；静脉注射) 不会显著改变 SNC 或 VTA 中自发性多巴胺 (DA) 神经元的发放频率或模式。单次腹腔注射 0.1 或 0.3 mg/kg，Cutamesine 不会改变自发活动的 SNC 和 VTA DA 神经元的数量^[3]。
单次腹腔注射 1 mg/kg Cutamesine 则分别显著减少和增加自发活动的 SNC 和 VTA DA 神经元的数量^[3]。
重复腹腔注射 0.3 和 1 mg/kg Cutamesine (每天注射一次，持续 21 天) 可显著增加自发活动的 VTA DA 神经元的数量^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

368.51

C₂₃H₃₂N₂O₂

165377-43-5

固体

Off-white to light yellow

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Lever JR, et al. Sigma1 and sigma2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse. 2006 May;59(6):350-8.  [Content Brief]

  [2]. Ono Y, et al. SA4503, a sigma-1 receptor agonist, suppresses motor neuron damage in in vitro and in vivo amyotrophic lateral sclerosis models. Neurosci Lett. 2014 Jan 24;559:174-8.  [Content Brief]

  [3]. Minabe Y, et al. Acute and chronic administration of the selective sigma1 receptor agonist SA4503 significantly alters the activity of midbrain dopamine neurons in rats: An in vivo electrophysiological study. Synapse. 1999 Aug;33(2):129-40.  [Content Brief]