Drug intelligence / Profile preview

PD149163

Development stage
Preclinical
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intraperitoneal, Subcutaneous
01

Overview

PD149163 is a synthetic, brain-penetrant agonist of the neurotensin receptor 1 (NTS1 or NTR1), developed as an analogue of the endogenous peptide neurotensin. It shows antipsychotic-like, anxiolytic-like, and antidepressant-like effects in animal models. The compound has demonstrated efficacy in reversing deficits in prepulse inhibition and reducing psychostimulant-induced hyperactivity, suppressing conditioned avoidance responses without inducing catalepsy, and modulating memory and social behaviors in rodent studies. In addition, PD149163 has shown anti-apoptotic and antioxidative properties in models of gastrointestinal tract injury, potentially by modulating toll-like receptor 4 (TLR4) activity. Studies suggest possible investigational use in schizophrenia, cognitive impairment, affective disorders, and gastrointestinal inflammatory or apoptotic conditions[1][3][4][5][7][8].

02

Targets

NTR1 (Nitroreductase-1)

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