| References: |
in 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. At concentrations of 1-10μM, SA4503 reduced SOD1(G93A)-induced cell death in a concentration-dependent manner.
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. 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. For the detailed information of SA4503 2HCl, the solubility of SA4503 2HCl in water, the solubility of SA4503 2HCl in DMSO, the solubility of SA4503 2HCl in PBS buffer, the animal experiment (test) of SA4503 2HCl, the cell expriment (test) of SA4503 2HCl, the in vivo, in vitro and clinical trial test of SA4503 2HCl, the EC50, IC50,and affinity,of SA4503 2HCl, For the detailed information of SA4503 2HCl, the solubility of SA4503 2HCl in water, the solubility of SA4503 2HCl in DMSO, the solubility of SA4503 2HCl in PBS buffer, the animal experiment (test) of SA4503 2HCl, the cell expriment (test) of SA4503 2HCl, the in vivo, in vitro and clinical trial test of SA4503 2HCl, the EC50, IC50,and affinity,of SA4503 2HCl, Please contact DC Chemicals. |
