SA 4503

SA 4503 is a sigma-1 (σ₁) receptor agonist that is selective for σ₁ over σ₂ receptors in a radioligand binding assay using guinea pig brain homogenates (K_is = 4.6 and 63 nM, respectively).^1,2 SA 4503 (10 μM) reduces light-induced cell death, decreases in σ₁ expression, disruption of the mitochondrial membrane potential, and activation of caspase-3/7 in murine 661W cells, effects that are blocked by the σ₁ receptor antagonist BD 1047 (Item No. 22928).² In vivo, SA 4503 (10 mg/kg) increases extracellular acetylcholine concentrations in the frontal cortex and improves step-through latency in a passive avoidance test in rats with scopolamine-induced memory impairment.³ SA 4503 reduces working and reference memory errors induced by a time delay and MK-801 (Item No. 10009019) in a radial arm maze in rats when administered at a dose of 0.3 mg/kg, effects which are ameliorated by the σ₁ antagonist NE-100 (Item No. 19642).⁴ Pre-administration of SA 4503 (500 μM) into the intravitreal space reduces light-induced thinning of the mouse retina outer nuclear layer by approximately 50%. ²

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1. Lever, J.R., Gustafson, J.L., Zu, R., et al. σ1 and σ2 receptor binding affinity and selectivity of SA4503 and fluoroethyl SA4503. Synapse 59(6), 350-358 (2006).

2. Shimazawa, M., Sugitani, S., Inoue, Y., et al. Effect of a sigma-1 receptor agonist, cutamesine dihydrochloride (SA4503), on photoreceptor cell death against light-induced damage. Exp. Eye. Res. 132, 64-72 (2015).

3. Matsuno, K., Senda, T., Kobayashi, T., et al. SA4503, a novel cognitive enhancer, with σ1 receptor agonistic properties. Behav. Brain Res. 83(1-2), 221-224 (1997).

4. Zou, L.-B., Yamada, K., Sasa, M., et al. Effects of σ1 receptor agonist SA4503 and neuroactive steroids on performance in a radial arm maze task in rats. Neuropharmacology 39(9), 1617-1627 (2000).