title: TRPV1 signaling: mechanistic understanding and therapeutic potential.
abstract: Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel gated by noxious heat, vanilloids and extracellular protons. TRPV1 is acting as an important signal integrator in sensory nociceptors under physiological and pathological conditions including inflammation and neuropathy. Because of its integrative signaling properties in response to inflammatory stimuli, TRPV1 agonists and antagonists are predicted to inhibit the sensation of ongoing or burning pain that is reported by patients suffering from chronic pain, therefore offering an unprecedented advantage in selectively inhibiting painful signaling from where it is initiated. In this article, we firstly summarize recent advances in the understanding of the role of TRPV1 in pain signaling, including a overview of clinical pharmacological trials using TRPV1 agonists and antagonists. Finally, we also present an update on the mechanistic understanding and controlling of hyperthermia caused by TRPU1 antagonists, and provide perspective for future study.
authors.affiliation: CPPS, DECS, AstraZeneca R&D, Sweden. rongshya@gmail.com
authors.forename: Rong
authors.initials: R
authors.lastname: Xia
authors.forename: Tarek A
authors.initials: TA
authors.lastname: Samad
authors.forename: Joan
authors.initials: J
authors.lastname: Btesh
authors.forename: Lin-Hua
authors.initials: LH
authors.lastname: Jiang
authors.forename: Ibrahim
authors.initials: I
authors.lastname: Kays
authors.forename: Louise
authors.initials: L
authors.lastname: Stjernborg
authors.forename: Niek
authors.initials: N
authors.lastname: Dekker
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D006801:Humans; D010146:Pain / Q000188:drug therapy* / Q000378:metabolism*; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship; D050916:TRPV Cation Channels / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*
chemical_list: D000700:Analgesics; D050916:TRPV Cation Channels; C494484:TRPV1 receptor