Design, synthesis and biological evaluation of new thiazole scaffolds as potential TRPM8 antagonists

Marsicano, Vincenzo; Arcadi, Antonio; Bianchini, Gianluca; Tomassetti, Mara; Aramini, Andrea

doi:10.1016/j.bmcl.2021.128392

Cited by 2 publications

(1 citation statement)

References 55 publications

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“…[75][76][77] Recent studies have been carried out to design, synthesize and biologically evaluate new thiazole scaffolds as potent antagonists of TRPM8. 78 Also, an assay has been developed for the rapid identification of TRPM8 antagonists employing automated patch clamp electrophysiology together with virtual screening. With this approach, nebivolol was found to be a potential TRPM8 inhibitor, and the structural modification of its structure can lay a foundation for developing new TRPM8 blockers.…”

Section: Trpm8 As a Drug Targetmentioning

confidence: 99%

A Comprehensive Review on the Regulatory Action of TRP Channels: A Potential Therapeutic Target for Nociceptive Pain

Anand,

Rajagopal

2023

J Exp Neurosci

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The transient receptor potential (TRP) superfamily of ion channels in humans comprises voltage-gated, non-selective cation channels expressed both in excitable as well as non-excitable cells. Four TRP channel subunits associate to create functional homo- or heterotetramers that allow the influx of calcium, sodium, and/or potassium. These channels are highly abundant in the brain and kidney and are important mediators of diverse biological functions including thermosensation, vascular tone, flow sensing in the kidney and irritant stimuli sensing. Inherited or acquired dysfunction of TRP channels influences cellular functions and signaling pathways resulting in multifaceted disorders affecting skeletal, renal, cardiovascular, and nervous systems. Studies have demonstrated the involvement of these channels in the generation and transduction of pain. Based on the multifaceted role orchestrated by these TRP channels, modulation of the activity of these channels presents an important strategy to influence cellular function by regulating intracellular calcium levels as well as membrane excitability. Therefore, there has been a remarkable pharmaceutical inclination toward TRP channels as therapeutic interventions. Several candidate drugs influencing the activity of these channels are already in the clinical trials pipeline. The present review encompasses the current understanding of TRP channels and TRP modulators in pain and pain management.

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Section: Trpm8 As a Drug Targetmentioning

confidence: 99%

A Comprehensive Review on the Regulatory Action of TRP Channels: A Potential Therapeutic Target for Nociceptive Pain

Anand,

Rajagopal

2023

J Exp Neurosci

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Discovery of (S)–N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist

Qiao

et al. 2022

European Journal of Medicinal Chemistry

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Design, synthesis and biological evaluation of new thiazole scaffolds as potential TRPM8 antagonists

Cited by 2 publications

References 55 publications

A Comprehensive Review on the Regulatory Action of TRP Channels: A Potential Therapeutic Target for Nociceptive Pain

A Comprehensive Review on the Regulatory Action of TRP Channels: A Potential Therapeutic Target for Nociceptive Pain

Discovery of (S)–N-(3-isopropylphenyl)-2-(5-phenylthiazol-2-yl)pyrrolidine-1-carboxamide as potent and brain-penetrant TRPV1 antagonist

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