title: Identification of N-[(5-{[(4-methylphenyl)sulfonyl]amino}-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl]-l-leucine (NTRC-824), a neurotensin-like nonpeptide compound selective for the neurotensin receptor type 2.
abstract: Compounds acting via the neurotensin receptor type 2 (NTS2) are known to be active in animal models of acute and chronic pain. To identify novel NTS2 selective analgesics, we searched for NTS2 selective nonpeptide compounds using a FLIPR assay and identified the title compound (NTRC-824, 5) that, to our knowledge, is the first nonpeptide that is selective for NTS2 versus NTS1 and behaves like the endogenous ligand neurotensin in the functional assay.
authors.affiliation: Center for Organic and Medicinal Chemistry, Research Triangle Institute , P.O. Box 12194, 3040 Cornwallis Road, Research Triangle Park, North Carolina 27709, United States.
authors.forename: James B
authors.initials: JB
authors.lastname: Thomas
authors.forename: Angela M
authors.initials: AM
authors.lastname: Giddings
authors.forename: Robert W
authors.initials: RW
authors.lastname: Wiethe
authors.forename: Srinivas
authors.initials: S
authors.lastname: Olepu
authors.forename: Keith R
authors.initials: KR
authors.lastname: Warner
authors.forename: Philippe
authors.initials: P
authors.lastname: Sarret
authors.forename: Louis
authors.initials: L
authors.lastname: Gendron
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Longpre
authors.forename: Yanan
authors.initials: Y
authors.lastname: Zhang
authors.forename: Scott P
authors.initials: SP
authors.lastname: Runyon
authors.forename: Brian P
authors.initials: BP
authors.lastname: Gilmour
mesh_terms: D000700:Analgesics / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007700:Kinetics; D007930:Leucine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008956:Models, Chemical; D015394:Molecular Structure; D010146:Pain / Q000503:physiopathology / Q000517:prevention & control*; D051381:Rats; D018028:Receptors, Neurotensin / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000502:physiology; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000700:Analgesics; C000593227:N-((5-(((4-methylphenyl)sulfonyl)amino)-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl)leucine; D018028:Receptors, Neurotensin; D013449:Sulfonamides; D007930:Leucine