Drug intelligence / Profile preview

2-(3,4-dihydroxybenzylidene)-4-methoxy-2,3-dihydro-1h-inden-1-one

Development stage
Preclinical
Lead developer
North-West University
Modality
Small Molecules
Administration
Oral
01

Overview

2-(3,4-dihydroxybenzylidene)-4-methoxy-2,3-dihydro-1h-inden-1-one (often abbreviated as 2-BI) is a non-xanthine benzylidene indanone derivative that functions as a dual antagonist of the A1 and A2A adenosine receptors. It demonstrates higher binding affinity for these targets compared to caffeine (A1 Ki(rat) = 42 nM and A2A Ki(rat) = 78 nM) and is being investigated for its antidiabetic properties. Studies in animal models indicate that 2-BI suppresses intestinal postprandial glucose absorption and reduces hyperglycemia, suggesting potential for diabetes management. Its mechanism involves competitive antagonism at both A1 and A2A adenosine receptors, distinct from traditional xanthine-based antagonists like caffeine. The compound’s drug-likeness has been evaluated using computational tools, which found it meets standard pharmaceutical property criteria. No commercial or clinical product based on this exact molecule is currently approved.

Other names
2-BI
02

Targets

ADORA2A (Adenosine A₂A Receptor)ADORA1 (Adenosine receptor A1 subtype)

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