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COMPOUND 51

Development stage: Preclinical
Modality: Small Molecules

Overview

COMPOUND 51 is a novel small molecule identified through docking-based virtual screening as a selective antagonist of the adenosine A2A receptor (AR). It exhibits high affinity for the A2A AR (Ki = 0.27 μM) and good selectivity over the A1 adenosine receptor. In vitro, COMPOUND 51 demonstrated antagonistic activity in cAMP measurements (IC50 = 1.80 μM). Preclinical studies in a haloperidol-induced catalepsy (HIC) rat model, relevant for Parkinson's disease, showed good efficacy at doses up to 30 mg/kg.

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