JNJ16259685,409345-29-5

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JNJ16259685

CAS No. : 409345-29-5

MCE 国际站：JNJ16259685

产品活性：JNJ16259685 是一种选择性的 mGlu1 receptor 拮抗剂，能够浓度依赖性地抑制 mGlu1 的突触的活化，IC₅₀ 值为 19 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: 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.

In Vivo: 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).

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