| Bioactivity | 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]. |
| Invitro | 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]. |
| 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]. Animal Model: |
| Name | JF-NP-26 |
| CAS | 2341841-03-8 |
| Formula | C30H28FN3O4 |
| Molar Mass | 513.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Font J, et al. Optical control of pain in vivo with a photoactive mGlu5 receptor negative allosteric modulator [published correction appears in Elife. 2018 Jan 08;7:]. Elife. 2017;6:e23545. Published 2017 Apr 11. |
JF-NP-26
CAS: 2341841-03-8 F: C30H28FN3O4 W: 513.56
JF-NP-26, an inactive photocaged derivative of raseglurant, is the first caged mGlu5 receptor negative allosteric modula
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