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Louis S Premkumar

Louis S Premkumar

Southern Illinois University School of Medicine, USA

Title: TRPV1: A target for next generation analgesics

Biography

Biography: Louis S Premkumar

Abstract

Transient Receptor Potential Vanilloid 1 (TRPV1) is a nociceptive ion channel activated by capsaicin, an ingredient in hot chili pepper. TRPV1 has been shown to be sensitized and over-expressed in the sensory neurons in chronic pain conditions. Therefore, TRPV1 is considered to be a potential target for developing analgesics. Several TRPV1 antagonists have been developed and proven to be effective in alleviating certain modalities of pain. Unfortunately, antagonism of TRPV1 in humans induces hyperthermia. Resiniferatoxin (RTX), a potent agonist of TRPV1 exhibits unique properties that can be utilized to treat chronic pain conditions. Intrathecal administration of RTX potently and selectively activates TRPV1 causing a depolarization block of the central nerve terminals in the short-term, and ablating TRPV1 containing central nerve terminals of the sensory neuron in the long-term at the level of the spinal cord. Finally, preventing nociceptive transmission at the level of the spinal cord using RTX will be a useful strategy in chronic, debilitating and intractable pain arising from large and inaccessible areas, such as malignancies of internal organs and bone.