Neurotensin(8-13)
(Synonyms: 神经降压素(8-13)) 目录号 : GC36729
A neuropeptide
Cas No.:60482-95-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | Binding assays are performed on whole HT-29 cells at confluence. A day before the assay, cells (106 cells/0.4 mL, equivalent to 0.3 mg protein) are placed in 48-well plates. A special binding buffer that includes protease inhibitors (50 mM HEPES, 125 mM NaCl, 7.5 mM KCl, 5.5 mM MgCl2, 1 mM EGTA, 5 g/L bovine serum albumin, 2 mg/L chymostatin, 100 mg/L soybean trypsin inhibitor, 50 mg/L bacitracin, pH 7.4) is used for the experiments. In inhibition studies, cells are incubated for 1 h at 37°C in triplicate with 25,000 cpm of 125I-NT and variable concentrations (0.001-3,000 nM) of unlabeled NT(8-13), unlabeled NT-VIII, or NT-VIII labeled with natRe (final volume of 0.2 mL per well). The cells are then washed twice with cold binding buffer and afterward are solubilized with 1N NaOH at 37°C (0.4 mL per well). The activity is determined in a γ-counter. In saturation studies, cells are incubated in triplicate with increasing concentrations (0.1-10 nM) of 99mTc(CO)3NT-VIII for 1 h at 37°C (final volume, 0.2 mL per well). The concentrations of total technetium (99+99mTc) are equivalent to 0.2-20 MBq 99mTc activity per well. After 2 washings with the same binding buffer as before, the cells are then solubilized with 1N NaOH at 37°C (0.4 mL per well). The bound radioactivity is measured in the γ-counter. Nonspecific binding is determined with 1 μM unlabeled NT(8-13)[1]. |
References: [1]. García-Garayoa E, et al. Preclinical evaluation of a new, stabilized neurotensin(8--13) pseudopeptide radiolabeled with (99m)tc. J Nucl Med. 2002 Mar;43(3):374-83. | |
Neurotensin (8-13) is a neuropeptide that corresponds to the C-terminal residues 8-13 of neurotensin that binds to rat synaptic membranes with a Ki value of 13 nM.1 It induces contraction of guinea pig ileum (EC50 = 25 nM) and induces contraction of rat fundus equipotently to full length neurotensin (EC50s = 1.29 and 1.58 nM, respectively).1,2 In vivo, neurotensin (8-13) has antinociceptive effects in a mouse tail pressure test (ED50 = 50 nmol per animal).3 It induces extracellular dopamine release in the prefrontal cortex in rats.4 Neurotensin (8-13) also decreases diastolic blood pressure in a dose-dependent manner in normotensive rats without affecting heart rate.5
1.Granier, C., van Rietschoten, J., Kitabgi, P., et al.Synthesis and characterization of neurotensin analogues for structure/activity relationship studies. Acetyl-neurotensin-(8--13) is the shortest analogue with full binding and pharmacological activitiesEur. J. Biochem.124(1)117-124(1982) 2.Huidobro-Toro, J.P., and Kullak, A.Excitatory neurotensin receptors on the smooth muscle of the rat fundus: Possible implications in gastric motilityBr. J. Pharmacol.84(4)897-910(1985) 3.Furuta, S., Kisara, K., Sakurada, S., et al.Structure-antinociceptive activity studies with neurotensinBr. J. Pharmacol.83(1)43-48(1984) 4.Sotty, F., Brun, P., Leonetti, M., et al.Comparative effects of neurotensin, neurotensin(8-13) and [D-Tyr11]neurotensin applied into the ventral tegmental area on extracellular dopamine in the rat prefrontal cortex and nucleus accumbensNeuroscience98(3)485-492(2000) 5.Di Paola, E.D., and Richelson, E.Cardiovascular effects of neurotensin and some analogues on ratsEur. J. Pharmacol.175(3)279-283(1990)
| Cas No. | 60482-95-3 | SDF | |
| 别名 | 神经降压素(8-13) | ||
| 分子式 | C38H64N12O8 | 分子量 | 816.99 |
| 溶解度 | Water: 50 mg/mL (61.20 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.224 mL | 6.12 mL | 12.2401 mL |
| 5 mM | 0.2448 mL | 1.224 mL | 2.448 mL |
| 10 mM | 0.1224 mL | 0.612 mL | 1.224 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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[3H]Neurotensin(8-13) binds in human brain to the same sites as does [3H]neurotensin but with higher affinity
J Neurochem 1988 Jan;50(1):131-7.PMID:2826683DOI:10.1111/j.1471-4159.1988.tb13239.x.
The binding of [3H]Neurotensin(8-13) to membranes from human frontal cortex at 0 degree C was time dependent, specific, saturable, and reversible. Saturation isotherms provided an equilibrium dissociation constant (KD) of 0.52 nM, and the maximal number of binding sites (Bmax) was 3.5 pmol/g original wet weight of tissue. Scatchard analysis yielded a straight line, and the Hill coefficient was equal to 1, a result indicating that [3H]Neurotensin(8-13) bound to single, noncoopertive sites. The KD values of several analogs of neurotensin determined in competition with [3H]Neurotensin(8-13) were similar to those previously determined in competition with [3H]neurotensin. The regional distribution of binding sites for [3H]Neurotensin(8-13) was also similar to that for [3H]neurotensin. These results suggest that [3H]Neurotensin(8-13) binds to the same sites as [3H]neurotensin and that [3H]Neurotensin(8-13) has a higher affinity than [3H]neurotensin for these sites in human brain.
Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity
ACS Med Chem Lett 2019 Nov 19;11(1):16-22.PMID:31938457DOI:10.1021/acsmedchemlett.9b00462.
Fluorescence-labeled receptor ligands have emerged as valuable molecular tools, being indispensable for studying receptor-ligand interactions by fluorescence-based techniques such as high-content imaging, fluorescence microscopy, and fluorescence polarization. Through application of a new labeling strategy for peptides, a series of fluorescent Neurotensin(8-13) derivatives was synthesized by attaching red-emitting fluorophores (indolinium- and pyridinium-type cyanine dyes) to carbamoylated arginine residues in Neurotensin(8-13) analogues, yielding fluorescent probes with high NTS1R affinity (pK i values: 8.15-9.12) and potency (pEC50 values (Ca2+ mobilization): 8.23-9.43). Selected fluorescent ligands were investigated by flow cytometry and high-content imaging (saturation binding, kinetic studies, and competition binding) as well as by confocal microscopy using intact CHO-hNTS1R cells. The study demonstrates the applicability of the fluorescent probes as molecular tools to obtain, for example, information about the localization of receptors in cells and to determine binding affinities of nonlabeled ligands.
Synthesis of Neurotensin(8-13)-phosphopeptide heterodimers via click chemistry
Bioorg Med Chem Lett 2010 Jun 1;20(11):3306-9.PMID:20452768DOI:10.1016/j.bmcl.2010.04.038.
Two Neurotensin(8-13)-containing peptide heterodimers were prepared via copper(I)-mediated click chemistry. The resulting peptide dimers could be obtained in 28-31% yield after HPLC purification. Neurotensin(8-13)-containing peptide dimers were used in an in vitro binding assay to determine binding affinity towards the Neurotensin receptor-1 (NTR1). The determined IC(50) values of 8.3 microM and 0.7 microM indicate only very low binding affinity of the Neurotensin(8-13)-containing peptide heterodimers towards the NTR1.
Neurotensin(8-13): comparison of novel analogs for stimulation of cyclic GMP formation in neuroblastoma clone N1E-115 and receptor binding to human brain and intact N1E-115 cells
Biochem Pharmacol 1989 Oct 1;38(19):3377-82.PMID:2554923DOI:10.1016/0006-2952(89)90637-0.
Neurotensin(8-13), the carboxyl-terminal portion of neurotensin, is 4-50 times more potent than native neurotensin in binding to intact neuroblastoma N1E-115 cells and human brain tissue and in stimulation of intracellular cyclic GMP production and inositol phospholipid hydrolysis in clone N1E-115 (Gilbert JA and Richelson E, Eur J Pharmacol 99: 245-246, 1984; Gilbert JA et al., Biochem Pharmacol 35: 391-397, 1986; Kanba KS et al., J Neurochem 46: 946-952, 1986; and Kanba KS and Richelson E, Biochem Pharmacol 36: 869-874, 1987). A series of novel analogs of neurotensin (8-13) was synthesized, and a structure-activity study was done comparing the abilities of these peptides to stimulate intracellular cyclic GMP production in intact neuroblastoma clone N1E-115 and to inhibit the binding of [3H]neurotensin to these cells and to membranal preparations from human brain. A direct correlation was found for each analog between its EC50 for biochemical activity and its KD for binding ability in studies with clone N1E-115. Furthermore, a strong correlation existed for each peptide between its KD for binding to neurotensin receptors on these cells and its KD for binding to neurotensin receptors in human brain tissue. In this study, the residues that were important to the biochemical and binding activities of neurotensin (8-13) proved to be identical to the amino acids that are necessary for the functional integrity of native neurotensin (Gilbert JA et al., Biochem Pharmacol 35: 391-397, 1986.
A novel tetrabranched Neurotensin(8-13) cyclam derivative: synthesis, 64Cu-labeling and biological evaluation
J Inorg Biochem 2011 Jun;105(6):821-32.PMID:21497581DOI:10.1016/j.jinorgbio.2011.02.011.
New macrocyclic 1,4,8,11-tetraazacyclotetradecane (cyclam) derivatives with 1, 2 and 4 Neurotensin(8-13) units 4, 5 and 7 have been synthesized. Compounds 4 and 5 were prepared by the reaction of non-stabilized Neurotensin(8-13) and cyclamtetrapropionic acid 2 using 1-ethyl-3-(3-dimethylaminocarbonyl)carbodiimide-hydrochloride and N-hydroxysulfosuccinimide. The tetrameric compound 7 was synthesized by Michael addition of Neurotensin(8-13) acrylamide 6 and cyclam 1. The copper(II) complexation behavior of 4, 5 and 7 was investigated by UV/visible spectrophotometry and shows that the metal center resides inside the N4 chromophore with additional apical interactions established with pendant arms. The novel tetrabranched NT(8-13) cyclam 7 with nanomolar neurotensin receptor 1 binding affinity was efficiently radiolabeled with (64)Cu under mild conditions. (64)Cu⊂7 showed slow transchelation in the presence of a large amount of cyclam as competing ligand, while it completely remains intact in the presence of EDTA. The in vivo behavior of (64)Cu⊂7 was studied in rats and mice. The metabolic stability in rodent models was high with a half-life of intact (64)Cu⊂7 in plasma of 34 min in rats and 60 min in the mice, respectively. The binding affinity was high enough to demonstrate in vivo binding of (64)Cu⊂7 to NTR1 overexpressing HT-29 tumor xenotransplants in nude mice. Regarding elimination, (64)Cu⊂7 showed a substantial renal and reticuloendothelial accumulation. On the other hand, metabolization of the compound in vivo with a resulting metabolite-postulated to be the (64)Cu-cyclam-tetraarginine complex-also showed long retention in the circulating blood, preventing a better contrast of tumor imaging.