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].

Exposure of the neurons to H₂O₂ induced cell death, while pretreatment with Cutamesine inhibits neuronal cell death. Cutamesine also reduces the activation of the MAPK/ERK pathway and down-regulated the ionotropic glutamate receptor, GluR1^[2].

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

In substantia nigra pars compacta (SNC) and ventral tegmental area (VTA) in anesthetized, male Sprague-Dawley rats, Cutamesine (0.01-1.28 mg/kg; iv) does not significantly alter the firing rate or pattern of spontaneously active dopamine (DA) neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of Cutamesine does not alter the number of spontaneously active SNC and VTA DA neurons^[3].
A single injection of 1 mg/kg i.p. of Cutamesine produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively^[3].
The repeated administration (one injection per day for 21 days) of 0.3 and 1 mg/kg i.p. of Cutamesine produced a significant increase in the number of spontaneously active VTA DA neurons^[3].

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

368.51

C₂₃H₃₂N₂O₂

165377-43-5

Solid

Off-white to light yellow

COC1=CC=C(CCN2CCN(CCCC3=CC=CC=C3)CC2)C=C1OC

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]