SR142948 is a potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM.
SR142948 antagonizes neurotensin-induced inositol monophosphate formation in HT 29 cells with IC50 of 3.9 nM.
SR142948 inhibits the turning behavior induced by neurotensin in mice, completely antagonizes neurotensin-evoked acetylcholine release in the rat striatum at 0.1 mg/kg.
SR142948 also blocks both hypothermia and analgesia induced by i.c.v. injection of neurotensin injection into the ventral tegmental area.
