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Neurotensin (trifluoroacetate salt)是一种由13个氨基酸组成的神经肽,具有神经递质、激素和神经调质功能。

Neurotensin (trifluoroacetate salt) Chemical Structure

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Description

Neurotensin (trifluoroacetate salt) is a neuropeptide composed of 13 amino acids, which functions as a neurotransmitter, hormone, and neuromodulator. Neurotensin (trifluoroacetate salt) lowers blood pressure, inhibits gastrointestinal motility and gastric acid secretion to regulate digestive function, while also modulating ceramide synthesis via the NTS-NTSR2 signaling pathway to reduce inflammation and regulate metabolism. Neurotensin (trifluoroacetate salt) can be used in research related to neuropsychiatric disorders (such as schizophrenia and Parkinson's disease) and metabolic diseases (such as obesity and metabolic-associated fatty liver disease)[1-4].

In vitro, Neurotensin (trifluoroacetate salt) (1μM) treated MKN-1 and MKN-45 gastric cancer cells for 5 minutes. Neurotensin (trifluoroacetate salt) activated the expression and activity of matrix metalloproteinase-9 (MMP-9) through the NTR1 receptor, promoting cell invasion and migration[5]. Neurotensin (trifluoroacetate salt) (0.1μM) treated Calu-3, NCI-H358, and NCI-H441 non-small cell lung cancer cells for 5 minutes. Neurotensin (trifluoroacetate salt) significantly increased HER3 tyrosine phosphorylation and promoted the formation of EGFR/HER3 and HER2/HER3 heterodimers[6].

In vivo, Neurotensin (trifluoroacetate salt) (1pg–25ng; single injection) was administered intracerebroventricularly to CD-1 mice. Neurotensin (trifluoroacetate salt) significantly antagonized the analgesic effect induced by morphine[7]. Neurotensin (trifluoroacetate salt) (10μg; single injection) was administered intrathecally to C57BL/6 mice. Neurotensin (trifluoroacetate salt) significantly alleviated thermal pain and formaldehyde-induced pain[8].

References:
[1] Staley J, Fiskum G, Davis TP, et al. Neurotensin (trifluoroacetate salt) elevates cytosolic calcium in small cell lung cancer cells. Peptides. 1989 Nov-Dec;10(6):1217-21.
[2] Ehlers RA, Zhang Y, Hellmich MR, et al. Neurotensin (trifluoroacetate salt)-mediated activation of MAPK pathways and AP-1 binding in the human pancreatic cancer cell line, MIA PaCa-2. Biochem Biophys Res Commun. 2000 Mar 24;269(3):704-8.
[3] Okamoto A, Nakanishi T, Tonai S, et al. Neurotensin (trifluoroacetate salt) induces sustainable activation of the ErbB-ERK1/2 pathway, which is required for developmental competence of oocytes in mice. Reprod Med Biol. 2024 Mar 20;23(1):e12571.
[4] Banerjee M, Song J, Yan B, et al. Neurotensin (trifluoroacetate salt) promotes hepatic steatosis by regulating lipid uptake and mitochondrial adaptation in hepatocytes. Cell Death Dis. 2025 Apr 27;16(1):347.
[5] Akter H, Park M, Kwon OS, et al. Activation of matrix metalloproteinase-9 (MMP-9) by Neurotensin (trifluoroacetate salt) promotes cell invasion and migration through ERK pathway in gastric cancer. Tumour Biol. 2015 Aug;36(8):6053-62.
[6] Moody TW, Ramos-Alvarez I, Jensen RT. Adding of Neurotensin (trifluoroacetate salt) to non-small cell lung cancer cells increases tyrosine phosphorylation of HER3. Peptides. 2022 Oct;156:170858.
[7] Holmes BB, Rady JJ, Smith DJ, et al. Supraspinal Neurotensin (trifluoroacetate salt)-induced antianalgesia in mice is mediated by spinal cholecystokinin. Jpn J Pharmacol. 1999 Feb;79(2):141-9.
[8] Barnwal A, Tamang R, Sanjeev Das, et al. Ponatinib delays the growth of solid tumours by remodelling immunosuppressive tumour microenvironment through the inhibition of induced PD-L1 expression. Br J Cancer. 2023 Oct;129(6):1007-1021.

Neurotensin (trifluoroacetate salt)是一种由13个氨基酸组成的神经肽,具有神经递质、激素和神经调质功能。Neurotensin (trifluoroacetate salt)可降低血压、抑制胃肠运动及胃酸分泌来调节消化功能,同时通过NTS-NTSR2信号通路调控神经酰胺合成以减少炎症和调节代谢。Neurotensin (trifluoroacetate salt)可用于神经精神疾病(如精神分裂症、帕金森病)和代谢疾病(如肥胖、代谢相关脂肪肝)的相关研究[1-4]

在体外,Neurotensin (trifluoroacetate salt)(1μM)处理MKN-1和MKN-45胃癌细胞5分钟。Neurotensin (trifluoroacetate salt)通过NTR1受体激活基质金属蛋白酶-9(MMP-9)的表达和活性,促进细胞侵袭和迁移[5]。Neurotensin (trifluoroacetate salt)(0.1μM)处理Calu-3、NCI-H358和NCI-H441非小细胞肺癌细胞5分钟。Neurotensin (trifluoroacetate salt)显著增加HER3酪氨酸磷酸化,同时促进EGFR/HER3和HER2/HER3异源二聚体形成[6]

在体内,Neurotensin (trifluoroacetate salt)(1pg-25ng;单次注射)侧脑室注射于CD-1小鼠。Neurotensin (trifluoroacetate salt)显著拮抗了吗啡诱导的镇痛作用[7]。Neurotensin (trifluoroacetate salt)(10μg;单次注射)鞘内注射于C57BL/6小鼠。Neurotensin (trifluoroacetate salt)显著减轻了热痛和福尔马林诱导的疼痛[8]

实验参考方法

Cell experiment [1]:

Cell lines

Calu-3, NCI-H358, and NCI-H441 cells (non-small cell lung cancer cell lines)

Preparation Method

Cells were cultured in RPMI-1640 medium containing 10% fetal bovine serum (FBS). When confluent, cells were washed with SIT medium (RPMI-1640 containing sodium selenite, bovine insulin and apo-transferrin) for 2 hours. Cells were treated with inhibitors (e.g., SR48692, mAb3481, PP2, GM6001, PD98059, LY294002, N-acetylcysteine or Tiron) for 30min. Then Neurotensin (trifluoroacetate salt) (0.1μM) or Neuregulin 1 (NRG1) was added.

Reaction Conditions

0.1μM; 5min

Applications

Neurotensin (trifluoroacetate salt) significantly increased tyrosine phosphorylation of HER3 in NSCLC cells. NTS addition to NCI-H441 cells resulted in the formation of EGFR/HER3 and HER2/HER3 heterodimers. Adding Neurotensin (trifluoroacetate salt) to NSCLC cells increased phosphorylation of ERK, HER3, and AKT. Neurotensin (trifluoroacetate salt) increased colony formation of NSCLC cells. The ability of Neurotensin (trifluoroacetate salt) to increase HER3 tyrosine phosphorylation was impaired by SR48692 (NTSR1 antagonist), monoclonal antibody 3481 (HER3 blocker), GM6001 (MMP inhibitor), PP2 (Src inhibitor), Tiron (superoxide scavenger), or N-acetylcysteine (antioxidant).

Animal experiment [2]:

Animal models

Male CD-1 mice (weighing 25 to 30g)

Preparation Method

Mice were administered Neurotensin (trifluoroacetate salt) (1pg to 25ng) intracerebroventricularly (i.c.v.) in a volume of 4μl under light halothane anesthesia, generally 10min before the tail flick test (TFT). Morphine was administered intrathecally (i.t.) 5min before the TFT.

Dosage form

1pg to 25ng; i.c.v.; single injection

Applications

Neurotensin (trifluoroacetate salt) significantly antagonized the antinociceptive (analgesic) action of morphine administered intrathecally. This antianalgesic action of Neurotensin (trifluoroacetate salt) was mediated by spinal cholecystokinin (CCK).

References:
[1] Moody TW, Ramos-Alvarez I, Jensen RT. Adding of Neurotensin (trifluoroacetate salt) to non-small cell lung cancer cells increases tyrosine phosphorylation of HER3. Peptides. 2022 Oct;156:170858..
[2] Holmes BB, Rady JJ, Smith DJ, et al. Supraspinal Neurotensin (trifluoroacetate salt)-induced antianalgesia in mice is mediated by spinal cholecystokinin. Jpn J Pharmacol. 1999 Feb;79(2):141-9.

化学性质

Cas No. SDF
分子式 C78H121N21O20•XCF3COOH 分子量 1672.9
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1 mM 597.8 μL 2.9888 mL 5.9776 mL
5 mM 119.6 μL 597.8 μL 1.1955 mL
10 mM 59.8 μL 298.9 μL 597.8 μL
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