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May 31, 2026Journal of Pharmacological Sciences0 citationsOpen Access

Luzindole and Ramelteon Block K V 4.2 Channels Independently of Melatonin Receptors

Luzindole and ramelteon share a melatonin receptor-independent blocking effect on voltage-gated potassium KV4.2 channels

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Authors

HKHibiki KuzuharaHMHiroki MishimaSFSawa Fujita

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Overview

Randomized trial examines KV4.2 inhibition by luzindole and ramelteon, indicating novel pharmacological actions of melatonin-related compounds.

Key Points

  • This study aims to investigate whether luzindole and ramelteon inhibit KV4.2 channels independent of melatonin receptors.
  • Assessed inhibition of KV4.2 channels using human embryonic kidney 293 cells expressing KV4.2 channels.
  • Performed whole-cell patch-clamp recordings to evaluate current inhibition by various compounds.
  • Compared effects of melatonin, luzindole, ramelteon, and melatonin biosynthetic precursors on KV4.2 currents.
  • Luzindole inhibited KV4.2 currents with an IC50 of 33 μM.
  • Ramelteon demonstrated inhibition of KV4.2 currents with an IC50 of 177 μM.
  • Melatonin biosynthetic precursors did not inhibit KV4.2 channels, indicating structural specificity for inhibition.

Cite This Study

Kuzuhara et al. (2026) studied this question.

synapsesocial.com/papers/6a1bcfb05783ba022b6fb9f0https://doi.org/10.1016/j.jphs.2026.05.008
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