Spatial intensity distribution analysis: studies of G Protein-coupled receptor oligomerization [PDF]
Spatial intensity distribution analysis (SpIDA) is a recently developed approach for determining quaternary structure information on fluorophore-labelled proteins of interest in situ. It can be applied to live or fixed cells and native tissue.
Marsango, Sara +3 more
core +1 more source
THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors
The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets ...
Stephen P H Alexander +154 more
wiley +1 more source
Cabergoline, dopamine D2 receptor agonist, prevents neuronal cell death under oxidative stress via reducing excitotoxicity. [PDF]
Several lines of evidence demonstrate that oxidative stress is involved in the pathogenesis of neurodegenerative diseases, including Parkinson's disease. Potent antioxidants may therefore be effective in the treatment of such diseases.
Haruki Odaka +7 more
doaj +1 more source
In contrast to the dose‐occupancy relationship in the treatment of schizophrenia, the minimal effective level of dopamine receptor 2 (D2R) blockade for antipsychotics in the treatment of bipolar depression is unknown. Lower doses aimed at reducing extrapyramidal side effects must be balanced against the need to retain the therapeutic benefit of D2R ...
Seth C. Hopkins +6 more
wiley +1 more source
The role of kinetic context in apparent biased agonism at GPCRs [PDF]
Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes and offers the prospect of designing pathway-specific drugs that avoid on-target side effects. This mechanism is usually
A Akinc +62 more
core +1 more source
Fast phasic release properties of dopamine studied with a channel biosensor [PDF]
Few other neurotransmitters are of as intense interest to neuropsychiatry and neurology as dopamine, yet existing techniques to monitor dopamine release leave an important spatiotemporal gap in our understanding. Electrochemistry and fluorescence imaging
Benz, Ann +6 more
core +2 more sources
O efeito estimulante da spiperona e da naloxana sob a maturação ovariana foram avaliados em fêmeas de Aegla uruguayana Schmitt, 1942 e, para isto, tais neuroreguladores foram incorporados ao alimento e administrados a uma dose de 10-8 mol/animal a cada ...
Daniela da S. Castiglioni +5 more
doaj +1 more source
Honey bee dopamine and octopamine receptors linked to intracellular calcium signaling have a close phylogenetic and pharmacological relationship. [PDF]
BACKGROUND: Three dopamine receptor genes have been identified that are highly conserved among arthropod species. One of these genes, referred to in honey bees as Amdop2, shows a close phylogenetic relationship to the a-adrenergic-like octopamine ...
Kyle T Beggs +2 more
doaj +1 more source
τBu₂SiF-Derivatized D₂-Receptor Ligands: The First SiFA-Containing Small Molecule Radiotracers for Target-Specific PET-Imaging [PDF]
The synthesis, radiolabeling and in vitro evaluation of new silicon-fluoride acceptor (SiFA) derivatized D-2-receptor ligands is reported. The SiFA-technology simplifies the introduction of fluorine-18 into target specific biomolecules for Positron ...
Bartenstein, Peter +10 more
core +2 more sources
An improved synthesis of (3-N-[11C]methyl)spiperone
An improved radiochemical synthesis of (3-N-[11C]methyl) spiperone is reported. The radiotracer was prepared by N-alkylation of spiperone in dimethylformamide in the presence of equimolar aqueous tetrabutylammonium hydroxide and was purified by semi-preparative reversed phase high performance liquid chromatography (C-18 HPLC). The average radiochemical
R F, Dannals +3 more
openaire +2 more sources

