7-tert-Butyl-6-(4-Chloro-Phenyl)-2-Thioxo-2,3-Dihydro-1HPyrido[2,3-d]Pyrimidin-4-One, a classic polymodal Inhibitor of TRVP1 with a reduced liability for hyperthermia, Is analgesic and ameliorates visceral hypersensitivity

Nash, M, McIntyre, P, Groarke, A, Lilley, E and Culshaw, A 2012, '7-tert-Butyl-6-(4-Chloro-Phenyl)-2-Thioxo-2,3-Dihydro-1HPyrido[2,3-d]Pyrimidin-4-One, a classic polymodal Inhibitor of TRVP1 with a reduced liability for hyperthermia, Is analgesic and ameliorates visceral hypersensitivity', The Journal of Pharmacology and Experimental Therapeutics, vol. 342, no. 2, pp. 389-398.


Document type: Journal Article
Collection: Journal Articles

Title 7-tert-Butyl-6-(4-Chloro-Phenyl)-2-Thioxo-2,3-Dihydro-1HPyrido[2,3-d]Pyrimidin-4-One, a classic polymodal Inhibitor of TRVP1 with a reduced liability for hyperthermia, Is analgesic and ameliorates visceral hypersensitivity
Author(s) Nash, M
McIntyre, P
Groarke, A
Lilley, E
Culshaw, A
Year 2012
Journal name The Journal of Pharmacology and Experimental Therapeutics
Volume number 342
Issue number 2
Start page 389
End page 398
Total pages 10
Publisher American Society for Pharmacology and Experimental Therapeutics
Abstract The therapeutic potential of transient receptor potential vanilloid type 1 (TRPV1) antagonists for chronic pain has been recognized for more than a decade. However, preclinical and clinical data revealed that acute pharmacological blockade of TRPV1 perturbs thermoregulation, resulting in hyperthermia, which is a major hurdle for the clinical development of these drugs. Here, we describe the properties of 7-tert-butyl-6-(4-chloro-phenyl)-2-thioxo-2,3- dihydro-1H-pyrido[2,3-d]pyrimidin-4-one (BCTP), a TRPV1 antagonist with excellent analgesic properties that does not induce significant hyperthermia in rodents at doses providing maximal analgesia
Subject Basic Pharmacology
DOI - identifier 10.1124/jpet.112.191932
Copyright notice © 2012 by The American Society for Pharmacology and Experimental Therapeutics
ISSN 0022-3565
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