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Items: 1 to 20 of 86

1.

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.

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-{[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.

4.

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
5.

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.

6.

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.

7.

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
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.

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.

10.

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
11.

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
12.

Synthesis and Characterization in Vitro and in Vivo of (l)-(Trimethylsilyl)alanine Containing Neurotensin Analogues.

Fanelli R, Besserer-Offroy É, René A, Côté J, Tétreault P, Collerette-Tremblay J, Longpré JM, Leduc R, Martinez J, Sarret P, Cavelier F.

J Med Chem. 2015 Oct 8;58(19):7785-95. doi: 10.1021/acs.jmedchem.5b00841. Epub 2015 Sep 16.

PMID:
26348111
13.

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
14.

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
15.

Targeting neurotensin receptors with agonists and antagonists for therapeutic purposes.

Kitabgi P.

Curr Opin Drug Discov Devel. 2002 Sep;5(5):764-76. Review.

PMID:
12630297
16.

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
17.

Spinal NTS1 receptors regulate nociceptive signaling in a rat formalin tonic pain model.

Roussy G, Dansereau MA, Doré-Savard L, Belleville K, Beaudet N, Richelson E, Sarret P.

J Neurochem. 2008 May;105(4):1100-14. doi: 10.1111/j.1471-4159.2007.05205.x. Epub 2007 Dec 25.

18.

Identification and functional characterization of a 5-transmembrane domain variant isoform of the NTS2 neurotensin receptor in rat central nervous system.

Perron A, Sarret P, Gendron L, Stroh T, Beaudet A.

J Biol Chem. 2005 Mar 18;280(11):10219-27. Epub 2005 Jan 6.

19.

NT69L, a novel analgesic, shows synergy with morphine.

Boules M, Shaw A, Liang Y, Barbut D, Richelson E.

Brain Res. 2009 Oct 19;1294:22-8. doi: 10.1016/j.brainres.2009.07.086. Epub 2009 Aug 3.

PMID:
19651107
20.

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

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