Abstract
Dopamine receptors are G-protein-coupled receptors (GPCRs), which are involved in a wide variety of physiological processes. Abnormalities in dopaminergic signal transduction are associated with many different diseases. Therefore, dopamine receptors are targets for variety of drugs involved in disorders like schizophrenia, Parkinson’s disease, depression and many others. In order to develop drugs with less side effects and better efficacy it is necessary to understand and characterize receptor-ligand interactions in further detail. In addition, measuring the on- and off-rates of different ligands provides important information about the kinetic profiles of potential drug candidates. We have applied fluorescence anisotropy (FA) assay to investigate kinetic properties and affinities of different ligands for dopamine D1 receptor. For that we have implemented budded baculoviruses as a source of recombinant protein (Veiksina et al., 2014). As a result, we have seen that fluorescent ligand Bodipy-FL-SKF-83566 is suitable for the pharmacological characterization of non-labelled dopaminergic ligands. The obtained results are in good agreement with the data obtained from the radioligand [3H]SCH 23390 binding experiments with the same baculovirus preparations. In conclusion, by using fluorescence based detection assay, we are now able to perform real-time monitoring of ligand binding. Obtained results demonstrate that fluorescence anisotropy based assay is applicable for the study of dopamine receptors and their ligands.
Highlights
Alzheimer’s disease (AD) is an incurable neurodegenerative disease characterized by progressive dementia
The results of the present study indicate that development of the neuronal hypoxic tolerance induced by the three-trial, in contrast to one-trial, mild hypoxic preconditioning is apparently largely associated with the activation of CREB, as well as brain-derived neurotrophic factor (BDNF) and Bcl-2 overexpression
No significant differences in serum level of Solubile form of RAGE (sRAGE) where found between rapidly progressing and slow progressing subgroup of multiple sclerosis (MS) patients.Our results suggest for the role of sRAGE in MS ethiopathogenesis, but we did not find any association of sRAGE in serum with the rate of MS disability progression
Summary
Alzheimer’s disease (AD) is an incurable neurodegenerative disease characterized by progressive dementia. The aim of the study was to characterize the effects of streptozocin (STZ)-indced diabetes on learning and memory of 5XFAD and wild-type (WT) mice in Morris water maze (MWM) at ages 2 and 6 months and on brain amyloid load. Existing evidence suggests GABAergic system is involved in pathophysiology of Alzheimer’s disease (AD) via inhibitory interneuron deficits (Verret et al, 2012) and decrease in functional GABAA receptors (Limon et al, 2012). Our concept: low doses of muscimol may prevent learning/memory deficits in intracerebroventricular (icv) streptozocin (STZ)-induced AD nontransgenic rat model. The Sigma-1 receptor is a chaperone protein that modulates intracellular calcium signalling of the endoplasmatic reticulum and is involved in learning and memory processes.The aim of the present study was to compare in vitro Ca2+ concentration modulating activity and in vivo behavioural effects of enantiomers of methylphenylpiracetam, a novel positive allosteric modulator of Sigma-1 receptors
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