Targeting TRPV1 for Analgesic Effects - Click here

Transient Receptor Potential Vanilloid 1 (TRPV1) is a non-selective cation channel expressed predominantly on nociceptive sensory neurons. It is activated by heat (>43 °C), acidic pH, capsaicin, and inflammatory mediators, making it a key mediator of inflammatory and neuropathic pain.

Analgesic strategies targeting TRPV1 include TRPV1 antagonists, which block channel activation and reduce nociceptor sensitization, and TRPV1 agonists (e.g., capsaicin), which induce prolonged desensitization or functional defunctionalization of pain fibers. These approaches have shown efficacy in managing chronic pain, inflammatory pain, and orofacial pain conditions.

In dentistry, TRPV1 modulation is being explored for dental pain control, pulpal inflammation, and temporomandibular disorders. However, clinical application is limited by challenges such as hyperthermia and altered heat sensation associated with systemic TRPV1 blockade.