SR 142948 TFA 

SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC₅₀s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC₅₀ of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders^[1][2].

SR 142948 (1 µM; 90 分钟) TFA 抑制 CHO-hNT1-R 细胞中 c-fos 和 krox24 的表达^[1]。
SR 142948 (0-1 µM; 1 小时) TFA 通过抑制 [¹²⁵I-Tyr³]NT 与 h-NTR1-CHO 和 HT 29 细胞膜的结合表现出良好的拮抗活性，IC₅₀ 分别为 1.19 和 0.32 nM^[2]。
SR 142948 (0-1 µM; 30 分钟) TFA 以浓度依赖性方式拮抗 h-NTR1-CHO 和 HT 29 细胞中 NT 刺激的 IP1 的产生^[2]。
SR 142948 (1, 10 nM; 60-80 秒) TFA 拮抗 h-NTR1-CHO 细胞中 NT 刺激的细胞内钙动员^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SR 142948 (2 µg/kg; 口服; 单次) TFA 抑制 NT (10 pg/小鼠) 诱导的转向行为^[2]。
SR 142948 (0.01, 0.03, 0.3 mg/kg; 腹腔注射; 单次) TFA 以剂量依赖性方式阻止 NT (100 nM) 产生的 ACh 释放增强^[2]。
SR 142948 (90-10 mg/kg; 口服; 单次) TFA 部分但显着地阻断 NT 诱导的体温过低 (大鼠 2 mg/kg 时 53% 和小鼠 4 mg/kg 时 54%)^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

799.88

C₄₁H₅₂F₃N₅O₈

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Portier M, et al. Neurotensin type 1 receptor-mediated activation of krox24, c-fos and Elk-1: preventing effect of the neurotensin antagonists SR 48692 and SR 142948. FEBS Lett. 1998 Jul 31;432(1-2):88-93.  [Content Brief]

  [2]. Gully D, et al. Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12.  [Content Brief]