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2024_AngCheInt_Photoswitchable_GorostizaP.pdf (1.77 MB)

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2024-09-16

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cc by-nc (c) Camerin, Luisa et al, 2024
Si us plau utilitzeu sempre aquest identificador per citar o enllaçar aquest document: https://hdl.handle.net/2445/215169

Photoswitchable Carbamazepine Analogs for Non-Invasive Neuroinhibition In Vivo

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A problem of systemic pharmacotherapy is off-target activity, which causes adverse effects. Outstanding examples include neuroinhibitory medications like antiseizure drugs, which are used against epilepsy and neuropathic pain but cause systemic side effects. There is a need of drugs that inhibit nerve signals locally and on-demand without affecting other regions of the body. Photopharmacology aims to address this problem with light-activated drugs and localized illumination in the target organ. Here, we have developed photoswitchable derivatives of the widely prescribed antiseizure drug carbamazepine. For that purpose, we expanded our method of ortho azologization of tricyclic drugs to meta/para and to N-bridged diazocine. Our results validate the concept of ortho cryptoazologs (uniquely exemplified by Carbazopine-1) and bring to light Carbadiazocine (8), which can be photoswitched between 400-590 nm light (using violet LEDs and halogen lamps) and shows good drug-likeness and predicted safety. Both compounds display photoswitchable activity in vitro and in translucent zebrafish larvae. Carbadiazocine (8) also offers in vivo analgesic efficacy (mechanical and thermal stimuli) in a rat model of neuropathic pain and a simple and compelling treatment demonstration with non-invasive illumination.

Descripció

Matèries

Epilèpsia, Fotofarmacologia

Matèries (anglès)

Epilepsy, Photopharmacology

Citació

Camerin, Luisa; Maleeva, Galyna; Gomila, Alexandre M J; Suarez-Pereira, Irene; Matera, Carlo; Prischich, Davia; Opar, Ekin; Riefolo, Fabio; Berrocoso, (2024). Photoswitchable Carbamazepine Analogs for Non-Invasive Neuroinhibition In Vivo. Angewandte Chemie (International Ed. Print), (), e202403636-. DOI: 10.1002/anie.202403636

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Articles publicats en revistes (Institut de Bioenginyeria de Catalunya (IBEC))

Citació

CAMERIN, Luisa, MALIEIEVA, Galyna, GOMILA JUANEDA, Alexandre, SUÁREZ PEREIRA, Irene, MATERA, Carlo, PRISCHICH, Davia, OPAR, Ekin, RIEFOLO, Fabio, BERROCOSO, Esther, GOROSTIZA LANGA, Pablo ignacio. Photoswitchable Carbamazepine Analogs for Non-Invasive Neuroinhibition In Vivo. _Angewandte Chemie (International Ed. Print)_. 2024. Vol. 63, núm. 38. [consulta: 1 de desembre de 2025]. ISSN: 1521-3773. [Disponible a: https://hdl.handle.net/2445/215169]

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