SR142948A is a selective and reversible non-peptide neurotensin receptor antagonist capable of blocking hypothermia and analgesic effects induced by intracerebroventricular injection of NT, and capable of concentration- and volume-dependent blockade of NMDA-induced dopamine release.

Inositol monophosphate (IP₁) formation via NT receptor (HT29 cells):3.9  nM

SR142948A HCl showed potent NT receptor antagonism in HT29 cells and CHO cells expressing human NT receptors, inhibiting inositol monophosphate formation and calcium mobilization, respectively (IC₅₀ = 3.9 nM for IP₁ formation)[1].

The in vivo activity of SR142948A HCl was evaluated in rats via intraperitoneal injection (0.1–100 mg/kg) to assess the effects on antipsychotic-related behaviors. In the latent inhibition model (0.1–10 mg/kg), SR142948A HCl blocked the normal acquisition of stimulus inhibition, and in the isolation-induced PPI deficit model (100 mg/kg), SR142948A HCl prevented haloperidol- and quetiapine-induced recovery of prepulse inhibition, indicating interference with neurotensin-dependent antipsychotic effects[1].