SR 142948

SR 142948 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 antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 shows blood-brain permeability and can be used in study of psychiatric disorders^[1][2]. In Vitro:SR 142948 (1 µM; 90 min) inhibits expression of c-fos and krox24 in CHO-hNT1-R cells^[1].
SR 142948 (0-1 µM; 1 h) exhibits good antagonistic activity by inhibiting [¹²⁵I-Tyr³]NT binds to h-NTR1-CHO and HT 29 cell membranes, with IC₅₀s of 1.19 and 0.32 nM, respectively^[2].
SR 142948 (0-1 µM; 30 min) antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner^[2].
SR 142948 (1, 10 nM; 60-80 s) antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells^[2]. In Vivo:SR 142948 (2 µg/kg; p.o.; single) inhibits the turning behavior induced by NT (10 pg/mouse)^[2].
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner^[2].
SR 142948 (0-10 mg/kg; p.o.; single) partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)^[2].