Merging two arylamidoalkyl substituted phenylpiperazines as prototypical recognition
elements for dopamine D2-like receptors by oligoethylene glycol linkers led to a series of …

Haloperidol is a typical antipsychotic drug (APD) associated with an increased risk of
extrapyramidal side effects (EPSs) and hyperprolactinemia relative to atypical APDs such as …

The dopamine D3 receptor (D3R) was proposed as a therapeutic target for drug
development to treat drug abuse and addiction and neuropsychiatric disorders. Several D3R …

Predicting the three‐dimensional structure of ligand–receptor complexes involving G protein‐
coupled receptors (GPCRs) is still a challenging task in rational drug design. To evaluate the …

The development of bitopic ligands directed toward D2-like receptors has proven to be of
particular interest to improve the selectivity and/or affinity of these ligands and as an …

In the frame of the discussion of monoamine‐related GPCRs, a novel knowledge‐based
ligand design strategy is presented. The strategy is founded on the integration of both, the …

The determination of G protein-coupled receptor (GPCR) structures at atomic resolution has
improved understanding of cellular signaling and will accelerate the development of new …

Despite tremendous successes of GPCR crystallography, the receptors with available
structures represent only a small fraction of human GPCRs. An important role of the …

Starting from FAUC 365, a series of iodine substituted heteroaryl carboxamides has been
synthesized revealing high affinity and selectivity for the dopamine D3 receptor. Binding …

Molecular modeling methods have been applied to construct three-dimensional models for
dopaminergic ligand complexes with D2 and D4 receptor subtypes (D2DAR and D4DAR) …