"目錄號(hào): HY-14813
SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.
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UNC0642-SA4503 dihydrochloride-Dextromethorphan hydrobromide hydrate-Noscapine-PRE-084 hydrochloride-S1RA hydrochloride-4-IBP-BD-1047 dihydrobromide-Siramesine hydrochloride-BD1063 dhydrochloride-Anavex 2-73-CYR-101-Dimemorfan phosphate-Sigma-LIGAND-1-
生物活性
Description
SA4503(AGY-94806; Cutamesine) is a selective sigma 1 receptor(σ1R) agonist; high affinity for the sigma 1 receptor subtype labeled by (+)-[3H]pentazocine (IC50 = 17.4 +/- 1.9 nM); 100-fold less affinity for the sigma 2 receptor.IC50 value: 17.4 nM [1]Target: σ1R agonistin vitro: SA4503 showed little affinity for 36 other receptors, ion channels and second messenger systems. SA4503 significantly increased the KD value, but did not affect the Bmax value for specific (+)-[3H]pentazocine binding. SA4503 is a potent and selective agonist for the sigma 1 receptor subtype in the brain [1].? At concentrations of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a concentration-dependent manner [3].in vivo: The intravenous administration of SA4503 (0.01-1.28 mg/kg) did not significantly alter the firing rate or pattern of spontaneously active DA neurons in either the SNC or VTA. A single injection of either 0.1 or 0.3 mg/kg i.p. of SA4503 did not alter the number of spontaneously active SNC and VTA DA neurons. In contrast, a single injection of 1 mg/kg i.p. of SA4503 produced a significant decrease and increase in the number of spontaneously active SNC and VTA DA neurons, respectively[2]. SA4503 suppressed the progression of ALS in an SOD1(G93A) ALS mouse model. SA4503 did not affect the onset time of ALS. However, it significantly extended the survival time in the SOD1(G93A) mice compared with a vehicle-treated group [3].
Clinical Trial
M's Science Corporation
Depressive Disorder, Major
November 2007
Phase 2
M's Science Corporation
Ischemic Stroke
February 2008
Phase 2
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References
