Drug intelligence / Profile preview

CGS21680

Development stage
Preclinical
Lead developer
Novartis
Modality
Small Molecules
Administration
Intravenous, Intracerebroventricular, In Vivo Experimental Administration
01

Overview

CGS21680 is a highly selective and potent **adenosine A2A receptor agonist** that has been widely used in research to study neuronal transmission, anti-inflammatory effects, neuroprotection, and the modulation of behavioral responses in animal models. Mechanistically, CGS21680 binds to and activates the adenosine A2A receptor, resulting in downstream signaling that can enhance neurotrophic pathways (notably by modulating brain-derived neurotrophic factor/TrkB signaling), exhibit anti-inflammatory properties, and influence cardiovascular, neurological, and behavioral responses. While shown to be potentially therapeutic in animal models of Huntington's disease, Rett syndrome, and inflammation (such as reducing lung injury and neurotoxicity), it is not approved for therapeutic use in humans and remains a tool compound primarily for laboratory research[1][3][4][6][7].

Other names
4-[2-[[6-Amino-9-(N-ethyl-β-D-ribofuranuronamidosyl)-9H-purin-2-yl]amino]ethyl]benzenepropanoic acid hydrochlorideCGS 21680 hydrochlorideCGS21680 hydrochlorideCGS-21680 hydrochlorideCGS-21680CGS21680CGS 21680
02

Targets

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

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