Drug intelligence / Profile preview

JNJ-40255293

Development stage
Preclinical
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral
01

Overview

**JNJ-40255293** is a small molecule dual antagonist of the adenosine A2A and A1 receptors, with high affinity and selectivity for the A2A receptor (7.5 nM, 7-fold selectivity for A2A over A1)[1][3][5][9]. It was developed by Johnson & Johnson as a potential treatment for Parkinson’s disease due to its ability to reverse motor impairments caused by dopamine antagonism or depletion in preclinical models[1][3][5][7]. JNJ-40255293 dose-dependently enhances consolidated waking in EEG studies, reverses hypolocomotion and catalepsy, potentiates effects of dopaminergic drugs, and supports the therapeutic potential of dual adenosine receptor antagonism in central nervous system diseases. The drug did not affect dopamine or noradrenaline release in prefrontal cortex and striatum, but synergized with other Parkinson's therapies (L-DOPA) in animal models[1][3][5]. JNJ-40255293 has also been explored for potential use in circadian rhythm modulation[2].

02

Targets

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

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