Overview
- Labbe-Jullie, C. et al. (1998) J. Biol. Chem. 273, 16351.
- Thomas, J.B. et al. (2009) Bioorg. Med. Chem. Lett. 19.5, 1438.
Alomone Labs SR 48692 inhibits human NTS1 receptors expressed in CHO-K1 cells.Dose-response curve of hNTSR1 normalized inhibition by SR 48692 (#S-265). Cells were loaded with Fluo-8 dye, incubated with increasing concentrations of SR 48692, and stimulated with 3 nM neurotensin. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 0.52 µM.
SR 48692 is a potent and selective antagonist of neurotensin receptor 1 (NTR1/NTS1). The compound demonstrates hydrophobic and aromatic features1,2. SR 48692 has been shown to antagonize neurotensin receptor actions in intestinal preparations, thus considered to be a useful tool in studying the physiological role of neurotensin receptor in the digestive tract. in vitro studies show that SR 48692 antagonizes NT-induced dopamine release in guinea pig striatal slices and NT-stimulated Ca2+ mobilization in HT29 cells1. In guinea pig ileum preparations, the compound displays an IC50 value of 33.5 nM1.
The two neurotensin receptors, NTR1 and NTR2, belong to the family of G-protein-coupled receptors1,2. The receptors are expressed in the brain and gastrointestinal tract where they play a role in pain transmission and intestinal motility.
