Towards Multitargeted Ligands as Pain Therapeutics: Dual Ligands of the Cavα2δ‐1 Subunit of Voltage‐Gated Calcium Channel and the μ‐Opioid Receptor
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DOI: 10.1002/cmdc.202300473
Abstract: The synthesis and pharmacological activity of a new series of dual ligands combining activities towards the α2δ‐1 subunit of voltage‐gated calcium channels (Cavα2δ‐1) and the μ‐opioid receptor (MOR) as novel pain therapeutics are reported. A… read more here.
Keywords: pain therapeutics; voltage gated; opioid receptor; gated calcium ... See more keywords
Mirogabalin activates the descending noradrenergic system by binding to the α2δ-1 subunit of voltage-gated Ca2+ channels to generate analgesic effects.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of pharmacological sciences"
DOI: 10.1016/j.jphs.2021.01.002
Abstract: Gabapentinoids such as gabapentin and pregabalin, which bind specifically to the α2δ subunit of voltage-gated Ca2+ channels, are used for first-line treatment of neuropathic pain. Here, we examined the analgesic effect of mirogabalin besilate (referred… read more here.
Keywords: system; descending noradrenergic; gated ca2; analgesic effects ... See more keywords