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编 号:F076866
分子式:C23H26Br2N2O
分子量:506.27
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1mg
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生物活性:
TAN-67 (SB-205607) dihydrobromide is a potent and selective nonpeptidic δ-opioid receptor agonist with a Ki value of 0.647 nM. TAN-67 dihydrobromide has neuroprotective effect. TAN-67 dihydrobromide can be used in research of ischemic stroke.

体内研究:
TAN-67 (SB-205607; 1.5-4.5 mg/kg; i.v.; once) dihydrobromide 减少 I/R 引起的脑损伤的梗塞体积。TAN-67 (3 mg/kg; i.v.; once) dihydrobromide 改善 I/R 后的生存和神经行为表现。TAN-67 (3 mg/kg; i.v.; once; 成年 C57BL/6J 雄性小鼠) dihydrobromide 在早期时间点 (6 h) 增加总 APP 和成熟 APP (APPm) 水平和 APP 处理。Animal Model:Adult C57BL/6J male mice with I/R-caused brain injury
Dosage:1.5, 3.0, and 4.5 mg/kg
Administration:Intravenous injection; once
Result:Reduced infarct volume in a dose-dependent manner.
Animal Model:Adult C57BL/6J male mice with I/R-caused brain injury
Dosage:3.0 mg/kg
Administration:Intravenous injection; once
Result:Had rapidly functional recovery than the vehicle-treated mice.Reduced neuronal cell death.
Animal Model:Adult C57BL/6J male mice with transient middle cerebra artery occlusion (MCAO) ischemic stroke model
Dosage:3.0 mg/kg
Administration:Intravenous injection; once
Result:Increased both total APP and mature APP (APPm) levels.Reduced β-secretase activity.

体外研究:
TAN-67 (SB-205607) dihydrobromide 高效 (EC50 = 1.72 nM) 抑制毛喉素刺激的 cAMP 在由完整的中国仓鼠卵巢细胞表达的人 delta-阿片受体上的积累,但在人 mu-阿片受体上的效力较低 (EC50 = 1520 nM)由完整的 B82 小鼠成纤维细胞表达。
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