The effects of the TRPV1 antagonist SB-705498 on TRPV1 receptor-mediated activity and inflammatory hyperalgesia in humans

BA Chizh, MB O'Donnell, A Napolitano, J Wang… - Pain, 2007 - Elsevier
TRPV1 is a cation channel activated by a range of noxious stimuli and highly expressed in
nociceptive fibres. TRPV1 receptors are involved in pain and sensitisation associated with
tissue injury and inflammation; hence, TRPV1 antagonists are potentially useful for the
treatment of such pain states. SB-705498 is a potent, selective and orally bioavailable
TRPV1 antagonist with demonstrated efficacy in a number of preclinical pain models. In this
first-time-into-human study, we have investigated the pharmacodynamic and …