Drug intelligence / Profile preview

PZ-1262

Development stage
Preclinical
Lead developer
Maj Institute of Pharmacology Polish Academy of Sciences
Modality
Small Molecules
01

Overview

PZ-1262 is a novel small molecule antipsychotic drug candidate, specifically a 4-isoquinoline-sulfonamide analog of brexpiprazole. It displays a multitarget pharmacological profile, showing partial agonist activity at the 5-HT1A receptor, and antagonist activity at the dopamine D2 and D3 receptors as well as at the serotonin 5-HT2A, 5-HT6, and 5-HT7 receptors. In preclinical rodent models, PZ-1262 has demonstrated potential antidepressant, anxiolytic, and procognitive (cognitive-enhancing) effects, along with possible antipsychotic activity. The compound was designed to enhance 5-HT6 receptor antagonism, an action thought to confer cognitive benefits. The pharmacodynamic characteristics suggest activity relevant to schizophrenia and cognitive dysfunction. As of the latest data, development remains preclinical and no human studies have been reported[1][3][9].

02

Targets

HTR6 (5-hydroxytryptamine receptor 6)DRD3 (Dopamine receptor D3)DRD2 (Dopamine D2 Receptor)HTR2A (Serotonin receptor 5-HT2A)HTR7 (5-hydroxytryptamine receptor 7)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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