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JNJ16259685

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Chemical Structure| 409345-29-5 同义名 : -
CAS号 : 409345-29-5
货号 : A854175
分子式 : C20H23NO3
纯度 : 95%
分子量 : 325.401
MDL号 : MFCD08690525
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：
生物活性
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].
实验方案
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
参考文献

[1]Lavreysen H,et al. JNJ16259685, a highly potent, selective and systemically active mGlu1 receptor antagonist. Neuropharmacology. 2004 Dec;47(7):961-72.

[2]Navarro JF,et al. JNJ16259685, a selective mGlu1 antagonist, suppresses isolation-induced aggression in male mice. Eur J Pharmacol. 2008 May 31;586(1-3):217-20.

[3]Hodgson RA, et al. Characterization of the selective mGluR1 antagonist, JNJ16259685, in rodent models of movement and coordination. Pharmacol Biochem Behav. 2011 Apr;98(2):181-7.