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

نویسندگان

  • James B. Thomas
  • 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
چکیده

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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عنوان ژورنال:

دوره 57  شماره 

صفحات  -

تاریخ انتشار 2014