A selective σ1 receptor agonist (Kis = 4.6 and 63 nM for σ1 and σ2

SA 4503 – 25 mg

Brand:
Cayman
CAS:
165377-44-6
Storage:
-20
UN-No:
De Minimis - 3077 / 9

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 (Kis = 4.6 and 63 nM, respectively).{45146,45147} 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).{45147} 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.{45148} 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).{45149} 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%. {45147}  

 

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Description

A selective σ1 receptor agonist (Kis = 4.6 and 63 nM for σ1 and σ2, respectively); 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 at 10 μM; 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 at 10 mg/kg; reduces working and reference memory errors induced by a time delay and MK-801 in a radial arm maze in rats at 0.3 mg/kg; pre-administration into the intravitreal space reduces light-induced thinning of the mouse retina outer nuclear layer at 500 μM

Formal name: 1-[2-(3,4-dimethoxyphenyl)ethyl]-4-(3-phenylpropyl)-piperazine, dihydrochloride

Synonyms:  AGY 94806|Cutamesine

Molecular weight: 441.4

CAS: 165377-44-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Ophthalmology

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