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Cannabidiol is a TRPV3 (warmth-sensing receptor) ligand with an affinity of 12 micromolar

atara

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For years the whole topical cannabinoid thing didn't make sense to me. Cannabinoids act on the central nervous system! Surely they don't just by complete accident act on an entirely different peripheral nerve receptor that also reduces pain, right?


CBD activates human TRPV3 with an EC50 of 12.8 µM.

:doh:

TRPV3 is a warmth-sensing receptor that responds to warm temperatures below 40 C (104 F). It's common for topical analgesics to work via TRPV3. And while 12 micromolar doesn't sound like very strong affinity, when you have a topical preparation the concentration is much higher than in the brain. For example the affinity of capsaicin for TRPV1 is about 2.4 micromolar.

In English: CBD acts on peripheral nerves by stimulating the warmth-sensing receptor. This may explain the effect of CBD ointments.
 
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