Drug intelligence / Profile preview

coumarin-caged N6-cyclopentyladenosine

Development stage
Preclinical
Lead developer
Ghent University
Modality
Small Molecules
Administration
Intrathecal
01

Overview

Coumarin-caged N6-cyclopentyladenosine (cCPA or pcCPA) is a photopharmacological, photocaged derivative of the selective adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA). Developed by researchers at Ghent University, cCPA is designed to achieve precisely localized and timed release of CPA upon illumination with 405 nm light. The coumarin caging group, specifically 7-(diethylamino)-4-(hydroxymethyl)-2H-chromen-2-one (DEACM), masks the bioactivity of CPA, reducing its affinity for the adenosine A1 receptor by over 1000-fold. Upon light-triggered uncaging, CPA is released to activate adenosine A1 receptors, which modulate neurotransmission via pre- and post-synaptic routes. This approach is being investigated for the focal suppression of seizure activity in models of drug-resistant epilepsy, such as mesial temporal lobe epilepsy, while preserving functional neurotransmission through closed-loop optical control.

Other names
coumarin-caged CPAphotocaged CPAphotocaged N6-cyclopentyladenosine
02

Targets

ADORA1 (Adenosine receptor A1 subtype)

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