Neurotensin
Neurotensin is an endogenous tridecapeptide that exhibits antinociceptive, pro-inflammatory, and gastrointestinal motility modulating activities; it binds and activates neurotensin (NTS) receptors. 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 non-selective 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/18948533
| Cas No. |
39379-15-2 |
|---|---|
| Purity |
≥95% |
| Formula |
C78H122N21O20 |
| Formula Wt. |
1672.9 |
| IUPAC Name |
2-[[2-[[2-[[1-[2-[[2-[[1-[6-amino-2-[[4-amino-2-[[4-carboxy-2-[[3-(4-hydroxyphenyl)-2-[[4-methyl-2-[(5-oxopyrrolidine-2-carbonyl)amino]pentanoyl]amino]propanoyl]amino]butanoyl]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 |
| Solubility |
Soluble in water. |
| Appearance |
White to off white powder |
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.
