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June 27, 2026Pharmacological ResearchOpen Access

Carbamate-based cannabinoids uncover a conserved lipid-sensing pocket in nociceptive TRPA1 and TRPV1 channels

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Authors

TATala AmawiYKYuliya KolesnykovaMGMariana Ghantous

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Overview

Randomized trial explores dual TRPA1/TRPV1 agonists in nociceptive channels, suggesting new analgesics.

Key Points

  • The aim is to define the structural characteristics of cannabinoid interactions with nociceptive ion channels TRPA1 and TRPV1.
  • Used rational ligand design to modify cannabidiol (CBD) and cannabigerol (CBG).
  • Conducted calcium imaging and patch-clamp recordings to assess ion channel activation.
  • Employed site-directed mutagenesis and molecular docking to determine binding sites.
  • Carbamate derivatives significantly increased TRPV1 potency while maintaining TRPA1 activation.
  • Carbamate modifications showed channel selectivity without potentiating TRPV2.
  • Derived agonists activated nociceptive neurons in a TRPV1-dependent manner, confirmed by TRPV1 antagonist BCTC.

Cite This Study

Amawi et al. (2026) studied this question.

synapsesocial.com/papers/6a3f67aaaea7db3c1953f035https://doi.org/10.1016/j.phrs.2026.108319
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1BPS2026 – Synergistic modulation of TRPA1 ion channel by cannabidiol and oleocanthal: A pharmacological and mechanistic study2026
  2. 2BPS2026 – Targeting the TRPV1-calmodulin interaction: A potential strategy to treat inflammatory and neuropathic pain2026 · 1 citations
  3. 3BPS2026 – TRPV1 antagonism occurs through diverse structural mechanisms2026
  4. 4Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists2024 · 22 citations
  5. 5TRPV3 activation by different agonists accompanied by lipid dissociation from the vanilloid site2024 · 46 citations