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

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...

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Veröffentlicht in:Journal of medicinal chemistry 2014-09, Vol.57 (17), p.7472-7477
Hauptverfasser: Thomas, James B, Giddings, Angela M, Wiethe, Robert W, Olepu, Srinivas, Warner, Keith R, Sarret, Philippe, Gendron, Louis, Longpre, Jean-Michel, Zhang, Yanan, Runyon, Scott P, Gilmour, Brian P
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Sprache:eng
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Zusammenfassung: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm500857r