SR 142948 TFA is an orally active, selective non-peptide neurotensin receptor (NT) antagonist, displaying IC50 values of 1.19 nM in h-NTR1-CHO cells, 0.32 nM in HT-29 cells, and 3.96 nM in adult rat brain. In HT-29 cells, it counteracts NT-induced inositol monophosphate formation with an IC50 of 3.9 nM. It blocks NT-induced hypothermia, analgesia, and turning behavior in vivo and can cross the blood-brain barrier, making it useful for research in psychiatric disorders.

SR 142948 (1 µM; 90 minutes) TFA inhibits the expression of c-fos and krox24 in CHO-hNT1-R cells. At concentrations ranging from 0 to 1 µM over an hour, SR 142948 TFA displays significant antagonistic activity by inhibiting [125 I-Tyr 3]NT binding to h-NTR1-CHO and HT 29 cell membranes, with IC 50 values of 1.19 and 0.32 nM, respectively. Additionally, SR 142948 (0-1 µM; 30 minutes) TFA antagonizes NT-stimulated IP1 production in a concentration-dependent manner in h-NTR1-CHO and HT 29 cells. Furthermore, at 1 and 10 nM for 60-80 seconds, SR 142948 TFA counteracts NT-induced intracellular calcium mobilization in h-NTR1-CHO cells.

SR 142948 administered orally at a dose of (2 µg/kg) effectively inhibits NT-induced turning behavior in mice. When administered by intraperitoneal injection at doses of (0.01, 0.03, 0.3 mg/kg), SR 142948 suppresses ACh release enhancement caused by NT (100 nM) in a dose-dependent manner. At doses ranging from (10-90 mg/kg) given orally, SR 142948 partially but significantly blocks NT-induced hypothermia, reducing it by 53% in rats at (2 mg/kg) and by 54% in mice at (4 mg/kg).