Matches in SemOpenAlex for { <https://semopenalex.org/work/W2034458389> ?p ?o ?g. }
- W2034458389 endingPage "7468" @default.
- W2034458389 startingPage "7459" @default.
- W2034458389 abstract "An involvement of the transient receptor potential vanilloid (TRPV) 1 channel in the regulation of body temperature (T(b)) has not been established decisively. To provide decisive evidence for such an involvement and determine its mechanisms were the aims of the present study. We synthesized a new TRPV1 antagonist, AMG0347 [(E)-N-(7-hydroxy-5,6,7,8-tetrahydronaphthalen-1-yl)-3-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)acrylamide], and characterized it in vitro. We then found that this drug is the most potent TRPV1 antagonist known to increase T(b) of rats and mice and showed (by using knock-out mice) that the entire hyperthermic effect of AMG0347 is TRPV1 dependent. AMG0347-induced hyperthermia was brought about by one or both of the two major autonomic cold-defense effector mechanisms (tail-skin vasoconstriction and/or thermogenesis), but it did not involve warmth-seeking behavior. The magnitude of the hyperthermic response depended on neither T(b) nor tail-skin temperature at the time of AMG0347 administration, thus indicating that AMG0347-induced hyperthermia results from blockade of tonic TRPV1 activation by nonthermal factors. AMG0347 was no more effective in causing hyperthermia when administered into the brain (intracerebroventricularly) or spinal cord (intrathecally) than when given systemically (intravenously), which indicates a peripheral site of action. We then established that localized intra-abdominal desensitization of TRPV1 channels with intraperitoneal resiniferatoxin blocks the T(b) response to systemic AMG0347; the extent of desensitization was determined by using a comprehensive battery of functional tests. We conclude that tonic activation of TRPV1 channels in the abdominal viscera by yet unidentified nonthermal factors inhibits skin vasoconstriction and thermogenesis, thus having a suppressive effect on T(b)." @default.
- W2034458389 created "2016-06-24" @default.
- W2034458389 creator A5004281302 @default.
- W2034458389 creator A5024263633 @default.
- W2034458389 creator A5028661046 @default.
- W2034458389 creator A5031885749 @default.
- W2034458389 creator A5035715127 @default.
- W2034458389 creator A5049612467 @default.
- W2034458389 creator A5049963981 @default.
- W2034458389 creator A5052505787 @default.
- W2034458389 creator A5058314246 @default.
- W2034458389 creator A5072798669 @default.
- W2034458389 creator A5082545277 @default.
- W2034458389 creator A5084797229 @default.
- W2034458389 date "2007-07-11" @default.
- W2034458389 modified "2023-10-14" @default.
- W2034458389 title "Nonthermal Activation of Transient Receptor Potential Vanilloid-1 Channels in Abdominal Viscera Tonically Inhibits Autonomic Cold-Defense Effectors" @default.
- W2034458389 cites W1488329806 @default.
- W2034458389 cites W1511198581 @default.
- W2034458389 cites W1905053669 @default.
- W2034458389 cites W1965509871 @default.
- W2034458389 cites W1966691304 @default.
- W2034458389 cites W1970677487 @default.
- W2034458389 cites W1986693123 @default.
- W2034458389 cites W1988174555 @default.
- W2034458389 cites W1988375390 @default.
- W2034458389 cites W1992358268 @default.
- W2034458389 cites W1993958507 @default.
- W2034458389 cites W2005024194 @default.
- W2034458389 cites W2009880851 @default.
- W2034458389 cites W2022023122 @default.
- W2034458389 cites W2031223488 @default.
- W2034458389 cites W2038066873 @default.
- W2034458389 cites W2039605663 @default.
- W2034458389 cites W2042079933 @default.
- W2034458389 cites W2043328385 @default.
- W2034458389 cites W2050781058 @default.
- W2034458389 cites W2051613742 @default.
- W2034458389 cites W2055827598 @default.
- W2034458389 cites W2056653713 @default.
- W2034458389 cites W2064911033 @default.
- W2034458389 cites W2066445331 @default.
- W2034458389 cites W2067433745 @default.
- W2034458389 cites W2068168026 @default.
- W2034458389 cites W2080593687 @default.
- W2034458389 cites W2083557005 @default.
- W2034458389 cites W2104390997 @default.
- W2034458389 cites W2105155111 @default.
- W2034458389 cites W2105163313 @default.
- W2034458389 cites W2106207830 @default.
- W2034458389 cites W2107705149 @default.
- W2034458389 cites W2115592638 @default.
- W2034458389 cites W2117164307 @default.
- W2034458389 cites W2117227828 @default.
- W2034458389 cites W2123057791 @default.
- W2034458389 cites W2129900856 @default.
- W2034458389 cites W2132358997 @default.
- W2034458389 cites W2134742719 @default.
- W2034458389 cites W2144670126 @default.
- W2034458389 cites W2148506230 @default.
- W2034458389 cites W2149855043 @default.
- W2034458389 cites W2151665669 @default.
- W2034458389 cites W2152585394 @default.
- W2034458389 cites W2155584991 @default.
- W2034458389 cites W2159616120 @default.
- W2034458389 cites W2163841453 @default.
- W2034458389 cites W2166917110 @default.
- W2034458389 cites W2167124891 @default.
- W2034458389 cites W2600182017 @default.
- W2034458389 cites W4242045149 @default.
- W2034458389 cites W4294062439 @default.
- W2034458389 doi "https://doi.org/10.1523/jneurosci.1483-07.2007" @default.
- W2034458389 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/6672610" @default.
- W2034458389 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/17626206" @default.
- W2034458389 hasPublicationYear "2007" @default.
- W2034458389 type Work @default.
- W2034458389 sameAs 2034458389 @default.
- W2034458389 citedByCount "201" @default.
- W2034458389 countsByYear W20344583892012 @default.
- W2034458389 countsByYear W20344583892013 @default.
- W2034458389 countsByYear W20344583892014 @default.
- W2034458389 countsByYear W20344583892015 @default.
- W2034458389 countsByYear W20344583892016 @default.
- W2034458389 countsByYear W20344583892017 @default.
- W2034458389 countsByYear W20344583892018 @default.
- W2034458389 countsByYear W20344583892019 @default.
- W2034458389 countsByYear W20344583892020 @default.
- W2034458389 countsByYear W20344583892021 @default.
- W2034458389 countsByYear W20344583892022 @default.
- W2034458389 countsByYear W20344583892023 @default.
- W2034458389 crossrefType "journal-article" @default.
- W2034458389 hasAuthorship W2034458389A5004281302 @default.
- W2034458389 hasAuthorship W2034458389A5024263633 @default.
- W2034458389 hasAuthorship W2034458389A5028661046 @default.
- W2034458389 hasAuthorship W2034458389A5031885749 @default.
- W2034458389 hasAuthorship W2034458389A5035715127 @default.
- W2034458389 hasAuthorship W2034458389A5049612467 @default.
- W2034458389 hasAuthorship W2034458389A5049963981 @default.