Tianeptine Metabolite MC5

噻奈普汀的活性代谢物；在使用表达人类MOR而非人类DOR的HEK293T细胞的BRET测定中选择性诱导G蛋白活化（EC50s分别为0.454和>100µM）；在野生型小鼠的强迫游泳测试中降低不动性，但不会影响MOR基因敲除小鼠，表明在30mg/kg剂量下具有MOR依赖性抗抑郁样活性。An active metabolite of tianeptine; selectively induces G protein activation in BRET assays using HEK293T cells expressing human MOR over human DOR (EC50s = 0.454 and >100 µM, respectively); decreases immobility in the forced swim test in wild-type mice, but not MOR knockout mice, indicating MOR-dependent antidepressant-like activity at 30 mg/kg.分子式C19H20ClN2O4S • Na分子量430.9O=C(CCCCNC1C2=C(N(S(=O)(C3=CC(Cl)=CC=C31)=O)C)C=CC=C2)[O-].[Na+]