SA 4503

SA 4503 is a sigma-1 (sigma1) receptor agonist that is selective for sigma1 over sigma2 receptors in a radioligand binding assay using guinea pig brain homogenates (Kis = 4.6 and 63 nM, respectively). SA 4503 (10 µM) reduces light-induced cell death, decreases in sigma1 expression, disruption of the mitochondrial membrane potential, and activation of caspase-3/7 in murine 661W cells, effects that are blocked by the sigma1 receptor antagonist BD 1047 (Cay-22928). 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. SA 4503 reduces working and reference memory errors induced by a time delay and MK-801 (Cay-10009019) in a radial arm maze in rats when administered at a dose of 0.3 mg/kg, effects which are ameliorated by the sigma1 antagonist NE-100 (Cay-19642). 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%. Formal Name: 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)-piperazine, dihydrochloride. CAS Number: 165377-44-6. Synonyms: AGY 94806, Cutamesine. Molecular Formula: C23H32N2O2 . 2HCl. Formula Weight: 441.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: PBS (pH 7.2): 5 mg/ml. SMILES: COC(C=C1)=C(OC)C=C1CCN(CC2)CCN2CCCC3=CC=CC=C3.Cl.Cl. InChi Code: InChI=1S/C23H32N2O2.2ClH/c1-26-22-11-10-21(19-23(22)27-2)12-14-25-17-15-24(16-18-25)13-6-9-20-7-4-3-5-8-20,,/h3-5,7-8,10-11,19H,6,9,12-18H2,1-2H3,2*1H. InChi Key: XWOXAKBQEMQMFH-UHFFFAOYSA-N.