Cargando…
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
[Image: see text] 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 (NTR...
| Autores principales: | , , , , , , , , , , |
|---|---|
| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2014
|
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4161155/ https://www.ncbi.nlm.nih.gov/pubmed/25157640 http://dx.doi.org/10.1021/jm500857r |
| _version_ | 1782334496470728704 |
|---|---|
| author | 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. |
| author_facet | 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. |
| author_sort | Thomas, James B. |
| collection | PubMed |
| description | [Image: see text] 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. |
| format | Online Article Text |
| id | pubmed-4161155 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2014 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-41611552015-08-26 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 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. J Med Chem [Image: see text] 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. American Chemical Society 2014-08-26 2014-09-11 /pmc/articles/PMC4161155/ /pubmed/25157640 http://dx.doi.org/10.1021/jm500857r Text en Copyright © 2014 American Chemical Society Terms of Use (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) |
| spellingShingle | 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. 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 |
| title | 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 |
| title_full | 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 |
| title_fullStr | 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 |
| title_full_unstemmed | 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 |
| title_short | 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 |
| title_sort | 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 |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4161155/ https://www.ncbi.nlm.nih.gov/pubmed/25157640 http://dx.doi.org/10.1021/jm500857r |
| work_keys_str_mv | AT thomasjamesb identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT giddingsangelam identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT wietherobertw identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT olepusrinivas identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT warnerkeithr identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT sarretphilippe identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT gendronlouis identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT longprejeanmichel identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT zhangyanan identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT runyonscottp identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 AT gilmourbrianp identificationofn54methylphenylsulfonylamino3trifluoroacetyl1hindol1ylacetyllleucinentrc824aneurotensinlikenonpeptidecompoundselectivefortheneurotensinreceptortype2 |