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[Gln4]-Neurotensin

Neurotensin is a tridecapeptide that exhibits antinociceptive, pro-inflammatory, and gastrointestinal motility modulating activities. Neurotensin induces contractions in smooth muscle cells, playing a role in regulating digestive activity in vitro and in vivo. Additionally, neurotensin induces intracellular Ca2+ release, activating nonselective cation channels and altering pacemaker currents involved in gastrointestinal and colonic motility. In animal models, neurotensin displays sympatho-inhibitory activity, decreases blood pressure and heart rate. Neurotensin exerts its actions through activation of neurotensin receptors; activation of these receptors also stimulates orexin neurons, suggesting a role for neurotensin in mediation of reward, feeding, and wakefulness.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18830240

Cas No.

61445-54-3

Purity

≥95%

Formula

C78H122N22O19

Formula Wt.

1671.9

IUPAC Name

2-[[2-[[2-[[1-[2-[[2-[[1-[6-amino-2-[[4-amino-2-[[5-amino-2-[[3-(4-hydroxyphenyl)-2-[[4-methyl-2-[(5-oxopyrrolidine-2-carbonyl)amino]pentanoyl]amino]propanoyl]amino]-5-oxopentanoyl]amino]-4-oxobutanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoic acid


product targets : IRE1 inhibitors

Kleczkowska P, Lipkowski AW. Neurotensin and neurotensin receptors: characteristic, structure-activity relationship and pain modulation–a review. Eur J Pharmacol. 2013 Sep 15;716(1-3):54-60. PMID: 23500196.

Degolier TF, Brown DR, Duke GE, et al. Neurotensin and cholecystokinin contract gallbladder circular muscle in chickens. Poult Sci. 2013 Aug;92(8):2156-62. PMID: 23873564.

Furutani N, Hondo M, Kageyama H, et al. Neurotensin co-expressed in orexin-producing neurons in the lateral hypothalamus plays an important role in regulation of sleep/wakefulness states. PLoS One. 2013 Apr 19;8(4):e62391. PMID: 23620827.

Lee J, Kim YD, Park CG, et al. Neurotensin modulates pacemaker activity in interstitial cells of Cajal from the mouse small intestine. Mol Cells. 2012 May;33(5):509-16. PMID: 22441675.

Zogovic B, Pilowsky PM. Intrathecal neurotensin is hypotensive, sympathoinhibitory and enhances the baroreflex in anaesthetized rat. Br J Pharmacol. 2012 May;166(1):378-89. PMID: 22035146.

Law IK, Murphy JE, Bakirtzi K, et al. Neurotensin-induced proinflammatory signaling in human colonocytes is regulated by β-arrestins and endothelin-converting enzyme-1-dependent endocytosis and resensitization of neurotensin receptor 1. J Biol Chem. 2012 Apr 27;287(18):15066-75. PMID: 22416137.

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