JNJ16259685 is a selective antagonist at the mGlu1 receptors, and inhibits the synaptic activation of mGlu1 in a concentration-dependent manner with IC50 of 19 nM.
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描述 | JNJ16259685 robustly and entirely suppresses the increase in intracellular Ca2+ levels triggered by glutamate (30 μM) at the rat mGlu1a receptor, with an IC50 of 3.24±1.00 nM. JNJ16259685 also impedes the glutamate-prompted elevation in intracellular Ca2+ levels at the rat mGlu5a receptor with an IC50 of 1.31±0.39 μM. Moreover, JNJ16259685 obstructs glutamate-induced Ca2+ mobilization at the human mGlu5 receptor with an IC50 of 28.3±11.7 μM. JNJ16259685 does not show any agonist activity at any of the group I mGlu receptors[1]. |
Animal study | Administered intraperitoneally, JNJ16259685 at doses of 0.25, 0.5, 1, 2, 4, and 8 mg/kg notably diminishes the duration of digging behaviors, as well as threat and attack behaviors, when compared to the vehicle group[2]. At a dosage of 30 mg/kg, JNJ16259685 has a negligible impact on locomotor activity. It significantly decreases rearing behavior, exploration in new environments, and lever pressing for food rewards (in rats at 0.3 mg/kg and in mice at 1 mg/kg). When administered subcutaneously at 30 mg/kg, JNJ16259685 does not affect the reflexive startle responses to loud sounds or foot shocks in mice[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.07mL 0.61mL 0.31mL |
15.37mL 3.07mL 1.54mL |
30.73mL 6.15mL 3.07mL |
CAS号 | 409345-29-5 |
分子式 | C20H23NO3 |
分子量 | 325.401 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 105 mg/mL(322.68 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |