JNJ16259685

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ16259685是一种选择性mGluR1拮抗剂，以浓度依赖性方式抑制mGluR1的突触激活，IC50为19 nM。

JNJ16259685 is a selective mGluR1 antagonist, and inhibits the synaptic activation of mGluR1 in a concentration-dependent manner with IC50 of 19 nM.

JNJ16259685 potently and completely inhibits the glutamate (30 μM)-induced increase in intracellular Ca2+?concentrations at the rat mGlu1a receptor with an IC50?value of 3.24±1.00 nM. IC50?values for CPCCOEt and BAY 36-7620 are 17.8±10.3 μM and 161±38 nM, respectively. The potency of JNJ16259685 in blocking glutamate (30 μM)-induced Ca2+ mobilization at the human mGlu1a receptor is 1.21±0.53 nM (IC50?n=3). JNJ16259685 inhibits the glutamate (3 μM)-induced rise in intracellular Ca2+?concentrations at the rat mGlu5a receptor with an IC50?value of 1.31±0.39 μM (n=4). JNJ16259685 blocks glutamate (3 μM)-induced Ca2+?mobilization at the human mGlu5 receptor with an IC50?of 28.3±11.7 μM (n=4). JNJ16259685 does not exhibit agonist activity at any of the group I mGlu receptors.

JNJ16259685 (0.125, 0.25, 0.5, 1, 2, 4 and 8?mg/kg, i.p) significantly reduces the time spent in digging behaviours (0.25-8 mg/kg), threat (all doses) and attack, in comparison with vehicle group. JNJ16259685 (30 mg/kg) produces very minimal effects on locomotor activity. JNJ16259685 dramatically reduces rearing behavior, exploration of a novel environment and lever pressing for a food reward (rat: 0.3 mg/kg; mouse: 1 mg/kg). Subcutaneously administered JNJ16259685 (30 mg/kg) has no effect on reflexive startle responses to loud auditory stimuli or foot shock in mice. JNJ16259685 exhibits high potencies in occupying central mGlu1 receptors in the rat cerebellum and thalamus (ED50=0.040 and 0.014 mg/kg, respectively).

.TN.T 16259685

Neuroscience

GluR

mGluR1

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409345-29-5

325.4

C20H23NO3

>98% (HPLC)

DMSO : 100 mg/mL (307.31 mM)

O=C(C1=CC=C2N=C3C(CCCO3)=CC2=C1)[C@H]4CC[C@@H](OC)CC4

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(-20℃)

With Ice Pack

≥ 2 years