The Quantitative Structure− Activity Relationship (QSAR) approach has been applied to
model binding affinity and receptor subtype selectivity of human 5HT1E and 5HT1F …

Imbalance of the dopaminergic system is involved in various neurological and
neuropsychiatric disorders, for example, Parkinson's disease, schizophrenia, and drug …

G protein–coupled receptors (GPCRs) are intensely studied as drug targets and for their role
in signaling. With the determination of the first crystal structures, interest in structure-based …

The dopamine D3 receptor (D3R) is an important central nervous system target for treating
various neurological diseases. D3R antagonists modulate the improvement of …

G-protein-coupled receptors (GPCRs) are targets of more than 30% of marketed drugs.
Investigation on the GPCRs may shed light on upcoming drug design studies. In the present …

A series of analogues featuring a 6-methoxy-1, 2, 3, 4-tetrahydroisoquinolin-7-ol unit as the
arylamine “head” group of a classical D3 antagonist core structure were synthesized and …

The dopaminergic system is one of the most important neurotransmitter systems in the
central nervous system (CNS). It acts mainly by activation of the D1-like receptor family at the …

Starting from dopamine receptor ligand BP897, an interactive drug discovery process
leading to heterocyclic bioisosteres is demonstrated. The four step strategy involved a …

The dopamine D4 receptor (D4R) plays important roles in cognition, attention, and decision
making. Novel D4R-selective ligands have promise in medication development for …

G protein-coupled receptors (GPCRs) are hard to crystallize. However, attempts to predict
their structure have boomed as a result of advancements in crystallographic techniques …