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TRPV1 antagonists that cause hypothermia, instead of hyperthermia, in rodents: Compounds' pharmacological profiles, in vivo targets, thermoeffectors recruited and implications for drug development.
Garami A, Pakai E, McDonald HA, Reilly RM, Gomtsyan A, Corrigan JJ, Pinter E, Zhu DXD, Lehto SG, Gavva NR, Kym PR, Romanovsky AA. Garami A, et al. Acta Physiol (Oxf). 2018 Jul;223(3):e13038. doi: 10.1111/apha.13038. Epub 2018 Feb 16. Acta Physiol (Oxf). 2018. PMID: 29352512 Free PMC article.
Pharmacological blockade of the vanilloid receptor TRPV1 elicits marked hyperthermia in humans.
Gavva NR, Treanor JJ, Garami A, Fang L, Surapaneni S, Akrami A, Alvarez F, Bak A, Darling M, Gore A, Jang GR, Kesslak JP, Ni L, Norman MH, Palluconi G, Rose MJ, Salfi M, Tan E, Romanovsky AA, Banfield C, Davar G. Gavva NR, et al. Pain. 2008 May;136(1-2):202-10. doi: 10.1016/j.pain.2008.01.024. Epub 2008 Mar 11. Pain. 2008. PMID: 18337008 Clinical Trial.