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Título

Remote local photoactivation of morphine produces analgesia without opioid-related adverse effects

AutorLópez-Cano, Marc; Font, Joan CSIC ORCID; Aso, Ester; Sahlholm, Kristoffer; Cabré, Gisela; Giraldo, Jesús; De Koninck, Yves; Hernando, Jordi CSIC ORCID; Llebaria, Amadeu CSIC ORCID; Fernández-Dueñas, Víctor; Ciruela, Francisco
Palabras claveOpioid-based drugs
Fecha de publicación6-ago-2021
EditorBritish Pharmacological Society
CitaciónBritish Journal of Pharmacology (2021)
ResumenBackground and Purpose Opioid-based drugs are the gold standard medicines for pain relief. However, tolerance and several side effects (i.e. constipation and dependence) may occur upon chronic opioid administration. Photopharmacology is a promising approach to improve the benefit/risk profiles of these drugs. Thus, opioids can be locally activated with high spatiotemporal resolution, potentially minimizing systemic-mediated adverse effects. Here, we aimed at developing a morphine photo-derivative (photocaged morphine), which can be activated upon light irradiation both in vitro and in vivo. Experimental Approach Light-dependent activity of pc-morphine was assessed in cell-based assays (intracellular calcium accumulation and electrophysiology) and in mice (formalin animal model of pain). In addition, tolerance, constipation and dependence were investigated in vivo using experimental paradigms. Key results In mice, pc-morphine was able to elicit antinociceptive effects, both using external light-irradiation (hind paw) and spinal cord implanted fibre-optics. In addition, remote morphine photoactivation was devoid of common systemic opioid-related undesired effects, namely, constipation, tolerance to the analgesic effects, rewarding effects and naloxone-induced withdrawal. Conclusion and Implications Light-dependent opioid-based drugs may allow effective analgesia without the occurrence of tolerance or the associated and severe opioid-related undesired effects.
Versión del editorhttps://doi.org/10.1111/bph.15645
URIhttp://hdl.handle.net/10261/251658
DOI10.1111/bph.15645
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