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Science of TRPV1 Agonism

An agonist is a substance which activates a receptor.

TRPV1 (transient receptor potential vanilloid 1) receptors initiate the activity of specialized nerve-cell endings called nociceptors (from the Latin noci-, meaning hurtful) that are responsible for the sensation of pain. TRPV1 receptors are activated by environmental stimuli such as heat or acidosis, and agonists such as capsaicin or lipids.

In people with chronic pain, nociceptors in the skin sometimes become hyperactive, continuously transmitting pain signals to the spinal cord-even in the absence of painful stimuli. However, over stimulation of TRPV1 receptors by exposure to an agonist such as capsaicin can cause these hyperactive nociceptors to become non-functional and reduce their ability to send pain signals. This impaired function may continue for weeks before the nociceptors return to their pre-treatment activity levels and regain their ability to transmit pain signals.1



1 Nolano M, Simone DA, Wendelschafer-Crabb G, Johnson T. Hazen E, Kennedy WR. Topical capsaicin in humans: parallel loss of epidermal nerve fibers and pain sensation. Pain. 1999;81:135-145.