1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. JF-NP-26

JF-NP-26 

Cat. No.: HY-131019
Handling Instructions

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.

For research use only. We do not sell to patients.

JF-NP-26 Chemical Structure

JF-NP-26 Chemical Structure

CAS No. : 2341841-03-8

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Description

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[1].

IC50 & Target[1]

mGlu5 Receptor

 

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)[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult male C57BL/6J mice weighing 20-25 g (chronic constriction injury (CCI) model)[1]
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[1]
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).
Molecular Weight

513.56

Formula

C₃₀H₂₈FN₃O₄

CAS No.

2341841-03-8

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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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

JF-NP-26mGluRMetabotropic glutamate receptorsinflammatoryneuropathicpainintracellularcalciumriseirradiationlightphotoactivationInhibitorinhibitorinhibit

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JF-NP-26
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HY-131019
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