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

  • J Med Chem. 2014 Sep 11;57(17):7472-7. doi: 10.1021/jm500857r.
James B Thomas  1 ,  Angela M Giddings ,  Robert W Wiethe ,  Srinivas Olepu ,  Keith R Warner ,  Philippe Sarret ,  Louis Gendron ,  Jean-Michel Longpre ,  Yanan Zhang ,  Scott P Runyon ,  Brian P Gilmour
Affiliations
  • 1. Center for Organic and Medicinal Chemistry, Research Triangle Institute , P.O. Box 12194, 3040 Cornwallis Road, Research Triangle Park, North Carolina 27709, United States.
PMID: 25157640 DOI: 10.1021/jm500857r
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.

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