Focusing on the similarity and divergence of GPCR subtypes and their ligand interactions,
we generated dopamine D2, D3, and D4 receptor models based on the rhodopsin crystal …

Interest in structure-based G-protein-coupled receptor (GPCR) ligand discovery is huge,
given that almost 30% of all approved drugs belong to this category of active compounds …

Background: Selectively targeting dopamine receptors (DRs) has been a persistent
challenge in the last years for the development of new treatments to combat the large variety …

Multiple subtypes of dopamine receptors within the GPCR superfamily regulate neurological
processes through various downstream signaling pathways. A crucial question about the …

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 subtype 3 receptor (D3) is a promising therapeutic target for the treatment of
cocaine addiction, schizophrenia, Parkinson's disease, and other disorders, but little is …

In this study, we designed and synthesized heterobivalent ligands targeting heteromers
consisting of the metabotropic glutamate 5 receptor (mGluR5) and the dopamine D2 …

The binding site of the dopamine D2 receptor (D2R), like those of homologous rhodopsin-
like G protein-coupled receptors (GPCRs) that bind small molecules, is contained within a …

We previously reported on the synthesis of substituted phenyl-4-hydroxy-1-piperidyl indole
analogues with nanomolar affinity at D2 dopamine receptors, ranging from 10-to 100-fold …

Introduction: Dopamine is a neurotransmitter widely distributed in both the periphery and the
central nervous system (CNS). Its physiological effects are mediated by five closely related G …