SR 142948 dihydrochloride_product_DataBase

Bioactivity

SR 142948 dihydrochloride 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 dihydrochloride antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 dihydrochloride blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 dihydrochloride shows blood-brain permeability and can be used in study of psychiatric disorders[1][2].

Invitro

SR 142948 (1 µM; 90 分钟) dihydrochloride 抑制 CHO-hNT1-R 细胞中 c-fos 和 krox24 的表达[1]。SR 142948 (0-1 µM; 1 小时) dihydrochloride 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) dihydrochloride 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) dihydrochloride 拮抗 h-NTR1-CHO 细胞中 NT 刺激的细胞内钙动员[2]。

In Vivo

SR 142948 (2 µg/kg; 口服; 单次) dihydrochloride 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) dihydrochloride 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) dihydrochloride 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]。 Animal Model:

Name

SR 142948 dihydrochloride

Formula

C39H53Cl2N5O6

Molar Mass

758.77

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

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

PeptideDB

SR 142948 dihydrochloride

CAS: F: C39H53Cl2N5O6 W: 758.77