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 | Zendy

James B. Thomas | Zendy; Angela M. Giddings | Zendy; Robert W. Wiethe | Zendy; O. Srinivas | Zendy; Keith R. Warner | Zendy; Philippe Sarret | Zendy; Louis Gendron | Zendy; JeanMichel Longpré | Zendy; Yanan Zhang | Zendy; Scott P. Runyon | Zendy; Brian P. Gilmour | Zendy

Open Access

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(s) -

James B. Thomas,

Angela M. Giddings,

Robert W. Wiethe,

O. Srinivas,

Keith R. Warner,

Philippe Sarret,

Louis Gendron,

JeanMichel Longpré,

Yanan Zhang,

Scott P. Runyon,

Brian P. Gilmour

Publication year - 2014

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm500857r

Subject(s) - neurotensin , chemistry , sulfonyl , chemical synthesis , stereochemistry , ligand (biochemistry) , neurotensin receptor , receptor , structure–activity relationship , pharmacology , biochemistry , neuropeptide , in vitro , organic chemistry , medicine , alkyl

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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