Research on dopamine (DA) and its receptors, and in particular the D2 receptor
subclass, has been an intriguing and fast developing scientific field in the past 35 years.
Methods of medicinal chemistry, molecular and structural biology as well as computational
chemistry were used in the studies of DA receptors (DRs). Early attempts to describe DRs
were based on a small amount of experimental data available and produced crude models at
best. Once crystal structures of bacteriorhodopsin, rhodopsine, various G-protein coupled
receptors, and finally D3 DR receptor became available, better and more detailed D2 DR receptor
models emerged. These models gave us an insight into the mechanism of ligand-receptor interactions,
and paved the way for the synthesis of new dopaminergic compounds, both agonists and antagonists and possible
drugs for the treatment of different imbalances of the dopaminergic system. This review covers the key
discoveries on the path to the creation of the D2 DR receptor model.
Keywords: 3D structure, computational chemistry, dopamine, GPCR, homology modeling, receptor.
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