JF-NP-26
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.
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- CAS No.: 2341841-03-8
- Formule: C30H28FN3O4
- Masse moléculaire:513.56
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Activité biologique
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mGlu5 Receptor |
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)[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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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[1].
Systemic administration and in vivo photoactivation of JF-NP-26 does not impair memory in mouse[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male C57BL/6J mice weighing 20-25 g (chronic constriction injury (CCI) model)[1]
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Dosage:10 mg/kg
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Administration:I.p.; irradiated at 405 nm (or dark) for 5 min
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Result:Significantly increased pain thresholds in CCI mice only after thalamic irradiation.
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Animal Model:Formalin animal model of pain adult male CD-1 mice[1]
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Dosage:10 mg/kg
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Administration:I.p.; at 405 nm light (or dark) for 5 min
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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).
Chemical Information
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CAS No. 2341841-03-8
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Masse moléculaire 513.56
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Formule C30H28FN3O4
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SMILES
O=C(OCC(C1=CC=C(N(CC)CC)C=C1O2)=CC2=O)NC3=C(C)C=C(C)N=C3C#CC4=CC=CC(F)=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JF-NP-26 Related Classifications
HY-131019 Related Classifications
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