Transient Receptor Potential Vanilloid 1 in Acute Pain: A Literature Review

Abstract

Transient Receptor Potential Vanilloid 1 (TRPV1) is a protein that functions as a non-selective channel receptor that is widely expressed in skin tissue, including keratinocytes, peripheral sensory nerve fibers, and immune cells. Several structural features of TRPV1 are involved in heat-induced activation, where stimulation of TRPV1 elicits a burning sensation, reflecting the receptor's important role in pain. A TRPV1- mediated signalling pathway that functions as an endogenous pain resolution mechanism by inducing nuclear translocation of β-arrestin2 to minimize desensitization of μ-opioid receptors (MOR). TRPV1 agonists can reduce pain primarily by interfering with pain nerve conduction. Several TRPV1 antagonist drug candidates have failed in clinical trials because by interfering with the detection of the above-mentioned stimuli, they triggered serious side effects such as hyperthermia and painful impaired heat detection. In the case of agonists, systemic administration causes more severe side effects such as respiratory damage. Therefore, only topical preparations with limited effectiveness have been developed. The TRPV1 agonist capsaicin is currently the only one approved for the treatment of muscle, bone, neuropathic pain and migraine, and is only available as a low-concentration cream or as a transdermal patch.