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JF-NP-26

CAS No. : 2341841-03-8

MCE 站：JF-NP-26

产品活性：JF-NP-26 是 Raseglurant 的无活性光笼衍生物，也是个光笼 mGlu5 受体负性变构调节剂。在可见光波段 (405 nm) 用光脉冲激发 JF-NP-26。JF-NP-26 诱导自由行为动物炎症性和神经病理性疼痛模型的光依赖性镇痛作用。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: The authors assessed the JF-NP-26-mediated negative allosteric modulation of mGlu5 receptor-induced responses to the orthosteric agonist quisqualate, by using an inositol phosphate (IP) accumulation assay. while JF-NP-26 didn’t show activity in dark conditions, its negative allosteric modulator (NAM) activity is rescued upon 405 nm visible light illumination (pIC₅₀=7.1).
Agonist challenge induced a robust mGlu5 receptor-mediated intracellular calcium rise both in dark and under 405 nm illumination, which was blocked by raseglurant. JF-NP-26 is unable to restrain agonist-mediated signalling in dark conditions, it abolished mGlu5 receptor-mediated intracellular calcium accumulation upon 405 nm irradiation, thus demonstrating a light-dependent negative allosteric modulator activity.

In Vivo: JF-NP-26 (10 mg/kg; i.p.; irradiated at 405 nm (or dark) for 5 min) significantly increased pain thresholds in CCI mice only after thalamic irradiation.
JF-NP-26 (10 mg/kg; i.p.; at 405 nm light (or dark) for 5 min) shows light-dependent analgesic efficacy in neuropathic pain.
Systemic administration and in vivo photoactivation of JF-NP-26 does not impair memory in mouse.

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