Neurotensin(8-13)

A neuropeptide

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
1mg

￥512.00

410.00

- +
5mg

￥1025.00

820.00

- +
10mg

￥1775.00

1420.00

- +
25mg

￥3687.00

2950.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

Background

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 K_i 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)

Protocol

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].

参考文献:

[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.