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

Autor:	Scott P. Runyon, Keith R. Warner, Louis Gendron, Angela M. Giddings, Philippe Sarret, James B. Thomas, Srinivas Olepu, Yanan Zhang, Jean-Michel Longpré, Brian P. Gilmour, Robert W. Wiethe
Rok vydání:	2014
Předmět:	Functional assay Brief Article Stereochemistry Pain CHO Cells Binding Competitive 03 medical and health sciences chemistry.chemical_compound Cricetulus 0302 clinical medicine Leucine Cricetinae Drug Discovery Animals Humans Receptors Neurotensin Neurotensin receptor 030304 developmental biology Sulfonyl chemistry.chemical_classification Analgesics Sulfonamides 0303 health sciences Dose-Response Relationship Drug Molecular Structure biology Chinese hamster ovary cell biology.organism_classification Rats 3. Good health Kinetics Models Chemical chemistry Biochemistry Molecular Medicine 030217 neurology & neurosurgery Neurotensin
Zdroj:	Journal of Medicinal Chemistry
ISSN:	1520-4804 0022-2623
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb318d09c6d576ce0723f5e8858e8e46 https://doi.org/10.1021/jm500857r Zobrazit plný text záznamu