Subtype selective dopamine receptor ligands have long been sought after as therapeutic
and/or imaging agents for the treatment and monitoring of neurologic disorders. We report …

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 …

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 …

G protein-coupled receptors (GPCRs) are capable of downstream signaling through distinct
noncanonical pathways such as β-arrestins in addition to the canonical G protein-dependent …

We have previously shown that using agonist affinity at recombinant receptors selectively
expressed in clonal cells as the dependent variable in three-dimensional quantitative …

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 …

A combined modeling approach was used to identify structural factors that underlie the
structure–activity relationships (SARs) of full dopamine D2 receptor agonists and structurally …

Agonist affinity changes dramatically as a result of serine to alanine mutations (S193A,
S194A, and S197A) within the fifth transmembrane region of D2 dopamine receptors and …

The dopamine 3 (D3) subtype receptor has been implicated in several neurological
conditions, and potent and selective D3 ligands may have therapeutic potential for the …

Recent breakthroughs in crystallographic studies of G protein-coupled receptors (GPCRs),
together with continuous progress in molecular modeling methods, have opened new …