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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Analgesics / chemical synthesis
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Analgesics / chemistry
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Analgesics / pharmacology*
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Animals
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Binding, Competitive
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CHO Cells
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Cricetinae
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Cricetulus
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Dose-Response Relationship, Drug
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Humans
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Kinetics
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Leucine / analogs & derivatives*
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Leucine / chemical synthesis
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Leucine / chemistry
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Leucine / pharmacology
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Models, Chemical
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Molecular Structure
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Pain / physiopathology
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Pain / prevention & control*
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Rats
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Receptors, Neurotensin / agonists*
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Receptors, Neurotensin / antagonists & inhibitors*
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Receptors, Neurotensin / physiology
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Sulfonamides / chemical synthesis
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
Substances
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Analgesics
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N-((5-(((4-methylphenyl)sulfonyl)amino)-3-(trifluoroacetyl)-1H-indol-1-yl)acetyl)leucine
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Receptors, Neurotensin
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Sulfonamides
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Leucine