Document Report Card

ID: ALA3352657

Journal: J Med Chem

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.

Authors: Thomas JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP.

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.

CiteXplore: 25157640

DOI: 10.1021/jm500857r