AG-0029

**AG-0029** is a dual-action small molecule drug developed as a novel therapeutic agent for **Parkinson's disease**, designed to address both **motor and cognitive symptoms**. Its mechanism involves potent **agonist activity at dopamine D2/D3 receptors** and **antagonist activity at histamine H3 receptors**. AG-0029 exhibits subnanomolar affinity for the dopamine D2/D3 receptors (EC50 0.08 nM) and moderate antagonist affinity for histamine H3 receptors (IC50 111 nM). In preclinical studies, AG-0029 rapidly crosses the blood-brain barrier, efficiently engages its targets, and demonstrates significant occupancy at these receptors (up to 84% for striatal D2/D3 and 40% for H3 at relevant doses). The drug has shown anti-Parkinsonian efficacy and cognitive improvement in animal models[1][3][5][7].

Other names

AG-0029AG0029AG 0029