Shedding Light On Photo-Switchable Analgesics For Pain

Optogenetics and photopharmacology in pain research and therapeutics

“…Optogenetics in the last two decades had a pivotal role in the investigation of pain physiology both in the central and peripheral nervous systems (84). Photopharmacology emerged in the recent years as a potential new approach to be applied in pain research and treatment (91). In this section, we pass into exam all the development in pain research and the potential biological targets that have been unravelled with the aid of these approaches.…”

“…A more advanced, photopharmacological approach can then be exploited to increase the complexity and capability of research to devise novel approaches to pain modulation and analgesia that can then be translated into therapeutics. To date, only few photo-switchable regulators of nociception have been developed and even less have been described in an in vivo system (13,91). In terms of potential targets involved in the pain pathways, one of the most obvious classes is represented by ion channels.…”

“…They assemble as homo-and hetero-dimeric complexes and scaffold a variety of proteins. GPCRs are potentially involved in all physiological processes in eukaryotic organisms, including acute and chronic pain (91). Indeed, most of the potent analgesics currently in use act through the μ-opioid receptor.…”

Light-controlled calcium signalling in prostate cancer and benign prostatic hyperplasia

“…We talk about the prospects for the particular conveyance of light to these organs and the particular prerequisites for light-active drugs [71]. Photoswitchable drugs are in the pipeline and identified with ionotropic glutamate receptors; kinate receptors; AMPA receptors; metabotropic glutamate receptors, adrenergic receptors, muscarinic acetylcholine receptors, dopamine, histamine, and serotonin receptors; calcium and potassium channels; and a number of transporters [72]. Thebault et al revealed that alpha-1 adrenoceptors are directly regulating the activation of TRP-mediated Ca 2+ entry, with all the members of the signalling cascade of α1-adrenoceptors that serve as targets for therapeutic interventions of cell proliferation which is ultimately responsible for the growth of prostate cancer cells [67,73].…”

Precise modulation of neuronal activity with synthetic photoswitchable ligands

“…with cell-targeted CRISPR knock-ins[56]. Finally, some of the photopharmacology tools mentioned above show promise for applications in pain regulation via photoswitchable analgesia, a field in its infancy, and recently reviewed elsewhere[57]. …”