Drug intelligence / Profile preview

SCH 412348

Development stage
Discontinued
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

SCH 412348 is a **potent and highly selective small molecule antagonist of the adenosine A2A receptor**, developed for nervous system diseases, primarily **Parkinson's disease**. It acts by blocking adenosine A2A receptors, which are highly expressed in the striatopallidal neurons involved in the regulation of movement. Preclinical studies demonstrate that SCH 412348 increases locomotor activity, reverses catalepsy, and restores motor function in rodent and primate models of Parkinson's disease, with high selectivity for A2A over other adenosine receptor subtypes (>1000-fold, Ki = 0.6 nM). It has shown efficacy both as monotherapy and in combination with levodopa in animal models. Clinical development was led by Merck Sharp & Dohme (originally as part of Schering-Plough), but the program was discontinued after reaching Phase 2 clinical trials.[1][3][5]

02

Targets

ADORA2A (Adenosine A₂A Receptor)

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