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Items: 1 to 20 of 78

1.

Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.

Thomas JB, Giddings AM, Olepu S, Wiethe RW, Harris DL, Narayanan S, Warner KR, Sarret P, Longpre JM, Runyon SP, Gilmour BP.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):292-6. doi: 10.1016/j.bmcl.2014.11.047. Epub 2014 Nov 24.

2.

Identification of 1-({[1-(4-fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)cyclohexane carboxylic acid as a selective nonpeptide neurotensin receptor type 2 compound.

Thomas JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP.

J Med Chem. 2014 Jun 26;57(12):5318-32. doi: 10.1021/jm5003843. Epub 2014 Jun 5.

3.

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 JB, Giddings AM, Wiethe RW, Olepu S, Warner KR, Sarret P, Gendron L, Longpre JM, Zhang Y, Runyon SP, Gilmour BP.

J Med Chem. 2014 Sep 11;57(17):7472-7. doi: 10.1021/jm500857r. Epub 2014 Aug 26.

4.

The amide linker in nonpeptide neurotensin receptor ligands plays a key role in calcium signaling at the neurotensin receptor type 2.

Thomas JB, Giddings AM, Olepu S, Wiethe RW, Warner KR, Sarret P, Longpre JM, Runyon SP, Gilmour BP.

Bioorg Med Chem Lett. 2015;25(10):2060-4. doi: 10.1016/j.bmcl.2015.03.083. Epub 2015 Apr 3.

5.

Identification of 2-({[1-(4-Fluorophenyl)-5-(2-methoxyphenyl)-1H-pyrazol-3-yl]carbonyl}amino)tricyclo[3.3.1.13,7]decane-2-carboxylic Acid (NTRC-844) as a Selective Antagonist for the Rat Neurotensin Receptor Type 2.

Thomas JB, Vivancos M, Giddings AM, Wiethe RW, Warner KR, Murza A, Besserer-Offroy É, Longpré JM, Runyon SP, Decker AM, Gilmour BP, Sarret P.

ACS Chem Neurosci. 2016 Sep 21;7(9):1225-31. doi: 10.1021/acschemneuro.6b00097. Epub 2016 Jul 13.

PMID:
27359371
6.

Low-affinity neurotensin receptor (NTS2) signaling: internalization-dependent activation of extracellular signal-regulated kinases 1/2.

Gendron L, Perron A, Payet MD, Gallo-Payet N, Sarret P, Beaudet A.

Mol Pharmacol. 2004 Dec;66(6):1421-30. Epub 2004 Sep 10.

PMID:
15361549
7.

NTS1 and NTS2 mediate analgesia following neurotensin analog treatment in a mouse model for visceral pain.

Smith KE, Boules M, Williams K, Richelson E.

Behav Brain Res. 2012 Jun 15;232(1):93-7. doi: 10.1016/j.bbr.2012.03.044. Epub 2012 Apr 5.

PMID:
22504145
8.

Potent spinal analgesia elicited through stimulation of NTS2 neurotensin receptors.

Sarret P, Esdaile MJ, Perron A, Martinez J, Stroh T, Beaudet A.

J Neurosci. 2005 Sep 7;25(36):8188-96.

9.

Evidence for a role of NTS2 receptors in the modulation of tonic pain sensitivity.

Roussy G, Dansereau MA, Baudisson S, Ezzoubaa F, Belleville K, Beaudet N, Martinez J, Richelson E, Sarret P.

Mol Pain. 2009 Jul 6;5:38. doi: 10.1186/1744-8069-5-38.

10.

Pharmacology and functional properties of NTS2 neurotensin receptors in cerebellar granule cells.

Sarret P, Gendron L, Kilian P, Nguyen HM, Gallo-Payet N, Payet MD, Beaudet A.

J Biol Chem. 2002 Sep 27;277(39):36233-43. Epub 2002 Jun 25.

11.

The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.

Thomas JB, Navarro H, Warner KR, Gilmour B.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1438-41. doi: 10.1016/j.bmcl.2009.01.024. Epub 2009 Jan 15.

12.

Neurotensin NTS1 and NTS2 receptor agonists produce anxiolytic-like effects in the 22-kHz ultrasonic vocalization model in rats.

Steele FF 3rd, Whitehouse SC, Aday JS, Prus AJ.

Brain Res. 2017 Mar 1;1658:31-35. doi: 10.1016/j.brainres.2017.01.012. Epub 2017 Jan 12.

PMID:
28089664
13.

Impact of the proline residue on ligand binding of neurotensin receptor 2 (NTS2)-selective peptide-peptoid hybrids.

Held C, Hübner H, Kling R, Nagel YA, Wennemers H, Gmeiner P.

ChemMedChem. 2013 May;8(5):772-8. doi: 10.1002/cmdc.201300054. Epub 2013 Mar 26.

PMID:
23532897
14.

The partial agonist properties of levocabastine in neurotensin-induced analgesia.

Dubuc I, Remande S, Costentin J.

Eur J Pharmacol. 1999 Sep 17;381(1):9-12.

PMID:
10528128
15.

Characterization of neurotensin receptors.

Kitabgi P, Pélaprat D.

Curr Protoc Pharmacol. 2004 May;Chapter 1:Unit 1.29. doi: 10.1002/0471141755.ph0129s24.

PMID:
22294115
16.

Use of Molecular Modeling to Design Selective NTS2 Neurotensin Analogues.

Fanelli R, Floquet N, Besserer-Offroy É, Delort B, Vivancos M, Longpré JM, Renault P, Martinez J, Sarret P, Cavelier F.

J Med Chem. 2017 Apr 27;60(8):3303-3313. doi: 10.1021/acs.jmedchem.6b01848. Epub 2017 Apr 10.

PMID:
28368584
17.

Analgesic synergy of neurotensin receptor subtype 2 agonist NT79 and morphine.

Boules M, Johnston H, Tozy J, Smith K, Li Z, Richelson E.

Behav Pharmacol. 2011 Sep;22(5-6):573-81. doi: 10.1097/FBP.0b013e3283474a3a.

PMID:
21691202
18.

Spinal NTS2 receptor activation reverses signs of neuropathic pain.

Tétreault P, Beaudet N, Perron A, Belleville K, René A, Cavelier F, Martinez J, Stroh T, Jacobi AM, Rose SD, Behlke MA, Sarret P.

FASEB J. 2013 Sep;27(9):3741-52. doi: 10.1096/fj.12-225540. Epub 2013 Jun 11.

PMID:
23756650
19.

Neurotensin inhibits background K+ channels and facilitates glutamatergic transmission in rat spinal cord dorsal horn.

Kadiri N, Rodeau JL, Schlichter R, Hugel S.

Eur J Neurosci. 2011 Oct;34(8):1230-40. doi: 10.1111/j.1460-9568.2011.07846.x. Epub 2011 Sep 21.

PMID:
21936876
20.

NTS2-selective neurotensin mimetics with tetrahydrofuran amino acids.

Simeth NA, Bause M, Dobmeier M, Kling RC, Lachmann D, Hübner H, Einsiedel J, Gmeiner P, König B.

Bioorg Med Chem. 2017 Jan 1;25(1):350-359. doi: 10.1016/j.bmc.2016.10.039. Epub 2016 Nov 1.

PMID:
27842797

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