1、分子量488.91 溶解性(25C) DMSO 分子式C H F N O SHClWater CAS号353229-59-1Ethanol 储存条件3年 -20C 粉末状 生物活性 LY-487379 is a positive allosteric modulator of the metabotropic glutamate receptor mGluR2. EC= 1.7 M. LY-487379 shows no intrinsic agonist or antagonist activity at hmGluR2 and has no activity at human mGluR3
2、. LY-487379 markedly potentiates glutamate-stimulated 35SGTPS binding in a concentration- dependent manner at hmGluR2, shifting the glutamate dose-response curve leftward by 3-fold and increasing the maximum levels of 35SGTPS stimulation. LY- 487379 has anxiolytic effects in fear-potentiated startle
3、. This activity profile is useful in all symptom domains of schizophrenia. 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南) 小鼠大鼠兔豚鼠仓鼠狗 重量 (kg)0.020.151.80.40.0810 体表面积 (m )0.0070.0250.150.050.020.5 K 系数36128520 动物 A (mg/kg) = 动物 B (mg/kg) 动物 B的K 系数 动物 A的K 系数 例如,依据体表面积折算法,将白藜芦醇用于小鼠的剂量22.4 mg/kg 换算成大鼠的剂量,需要将22.4 mg/kg 乘以小鼠的K 系数(3),再除以大鼠的K 系数(6), 得到白藜芦醇用于大鼠的等效剂量为11.2 mg/kg。 LY-487379 hydrochloride 目录号M7881 化学数据 2119324 50 2 m m m mm