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编 号：F715357
分子式：C30H28FN3O4
分子量：513.56
分子式：C30H28FN3O4
分子量：513.56
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CAS No: 2341841-03-8
产品详情
生物活性：
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.
体内研究：
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.Animal Model:Adult male C57BL/6J mice weighing 20-25 g (chronic constriction injury (CCI) model)
Dosage:10 mg/kg
Administration:I.p.; irradiated at 405 nm (or dark) for 5 min
Result:Significantly increased pain thresholds in CCI mice only after thalamic irradiation.
Animal Model:Formalin animal model of pain adult male CD-1 mice
Dosage:10 mg/kg
Administration:I.p.; at 405 nm light (or dark) for 5 min
Result:Unable to promote antinociception in dark conditions, it elicited antinociception following direct hind paw irradiation both at phase I (5 min after formalin injection in the hind paw) and phase II (20–30 min after formalin injection).
体外研究：
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.
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modulator. Uncaging of JF-NP-26 is elicited with light pulses in the visible spectrum (405 nm). JF-NP-26 induces light-dependent analgesia in models of inflammatory and neuropathic pain in freely behaving animals.
体内研究：
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.Animal Model:Adult male C57BL/6J mice weighing 20-25 g (chronic constriction injury (CCI) model)
Dosage:10 mg/kg
Administration:I.p.; irradiated at 405 nm (or dark) for 5 min
Result:Significantly increased pain thresholds in CCI mice only after thalamic irradiation.
Animal Model:Formalin animal model of pain adult male CD-1 mice
Dosage:10 mg/kg
Administration:I.p.; at 405 nm light (or dark) for 5 min
Result:Unable to promote antinociception in dark conditions, it elicited antinociception following direct hind paw irradiation both at phase I (5 min after formalin injection in the hind paw) and phase II (20–30 min after formalin injection).
体外研究：
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.
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