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J Med Chem. 2014 Sep 11;57(17):7472-7. doi: 10.1021/jm500857r. Epub 2014 Aug 26.

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.

Author information

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.

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.

PMID:
25157640
PMCID:
PMC4161155
DOI:
10.1021/jm500857r
[Indexed for MEDLINE]
Free PMC Article

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