[3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.

Bianchi, Bruce R; El Kouhen, Rachid; Neelands, Torben R; Lee, Chih-Hung; Gomtsyan, Arthur; Raja, Shirish N; Vaidyanathan, Sriajan N; Surber, Bruce; McDonald, Heath A; Surowy, Carol S; Faltynek, Connie R; Moreland, Robert B; Jarvis, Michael F; Puttfarcken, Pamela S

Bianchi, Bruce R; El Kouhen, Rachid; Neelands, Torben R; Lee, Chih-Hung; Gomtsyan, Arthur; Raja, Shirish N; Vaidyanathan, Sriajan N; Surber, Bruce; McDonald, Heath A; Surowy, Carol S; Faltynek, Connie R; Moreland, Robert B; Jarvis, Michael F; Puttfarcken, Pamela S.

Affiliation

Bianchi BR; Department of Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, R4PM, AP9A/2, 100 Abbott Park Rd, Abbott Park, IL 60064-6123, USA.

J Pharmacol Exp Ther ; 323(1): 285-93, 2007 Oct.

Article in En | MEDLINE | ID: mdl-17660385

Subject(s)

Isoquinolines/pharmacology; TRPV Cation Channels/antagonists & inhibitors; Urea/analogs & derivatives; Animals; Binding, Competitive; CHO Cells; Calcium Signaling/drug effects; Cell Membrane/metabolism; Cricetinae; Cricetulus; Ganglia, Spinal/cytology; Ganglia, Spinal/metabolism; Humans; Isoquinolines/chemical synthesis; Isoquinolines/chemistry; Ligands; Molecular Structure; Neurons, Afferent/metabolism; Radioligand Assay; Rats; Recombinant Proteins/antagonists & inhibitors; Stereoisomerism; Transfection; Tritium; Urea/chemical synthesis; Urea/chemistry; Urea/pharmacology

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Collection: 01-internacional Database: MEDLINE Main subject: Urea / TRPV Cation Channels / Isoquinolines Limits: Animals / Humans Language: En Journal: J Pharmacol Exp Ther Year: 2007 Document type: Article Affiliation country: United States Country of publication: United States

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