Drug intelligence / Profile preview

compound 21c

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

Overview

Compound 21c is a potent and selective small molecule adenosine A2A receptor antagonist belonging to the bicyclic piperazine triazolotriazine class. Developed by Schering-Plough (now Merck & Co.) as a potential non-dopaminergic therapeutic for Parkinson's disease, it was designed to address the motor symptoms of the condition by modulating striatal neurotransmission. In preclinical studies, compound 21c demonstrated high affinity for the A2A receptor and exceptional selectivity over the A1 receptor. It is particularly noted for its improved metabolic stability compared to earlier analogs in the same chemical series. The compound has shown oral efficacy in rodent models of Parkinson's disease, such as the reversal of catalepsy, and has demonstrated the ability to antagonize adenosine-mediated behavioral effects at low doses.

Other names
bicyclic piperazine derivative of triazolotriazine
02

Targets

ADORA2A (Adenosine A₂A Receptor)

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