Search results for " Neurotransmitter"
showing 10 items of 62 documents
Synthesis and monoamine uptake inhibition of conformationally constrained 2β-carbomethoxy-3β-phenyl tropanes
2009
A series of 2beta-carbomethoxy-3beta-phenyl tropanes with conformationally constrained nitrogen substituents were synthesized as potential selective dopamine transporter ligands. These novel compounds were examined for their monoamine uptake inhibition potency at the human dopamine transporter (hDAT), the human serotonin transporter (hSERT) and the human noradrenalin transporter (hNET), stably expressed in human embryonic kidney cells (HEK). A SAR-study was conducted to determine the contribution of extended, 4-fluorinated, conformationally constrained C4 chains at the tropane nitrogen to human monoamine transporter affinity and selectivity.
Role of hydrophobicity on the monoamine receptor binding affinities of central nervous system drugs: a quantitative retention-activity relationships …
2004
Abstract Biological action and activity reflect an aspect of the fundamental physicochemical properties of the bioactive compounds. As an alternative to classical QSAR studies, in this work different quantitative retention–activity relationships (QRAR) models are proposed, which are able to describe the role of hydrophobicity on the binding affinity to different brain monoamine receptors (H 1 -histamine, α 1 -noradrenergic and 5-HT 2 -serotonergic) of different families of psychotherapeutic drugs. The retention of compounds is measured in a biopartitioning micellar chromatography (BMC) system using Brij-35 mobile phases. The adequacy of the QRAR models developed is due to the fact that both…
BDNF regulates spontaneous correlated activity at early developmental stages by increasing synaptogenesis and expression of the K+/Cl- co-transporter…
2003
Spontaneous neural activity is a basic property of the developing brain,which regulates key developmental processes, including migration, neural differentiation and formation and refinement of connections. The mechanisms regulating spontaneous activity are not known. By using transgenic embryos that overexpress BDNF under the control of the nestin promoter, we show here that BDNF controls the emergence and robustness of spontaneous activity in embryonic hippocampal slices. Further, BDNF dramatically increases spontaneous co-active network activity, which is believed to synchronize gene expression and synaptogenesis in vast numbers of neurons. In fact, BDNF raises the spontaneous activity of…
Psicobiologia dell'attaccamento
2008
In this work, the emotional and cerebral development of the individual is treated as a complex process, within which genetic and experiential factors interact; equal focus is given to these factors as is through the interactions of both that the human brain achieves full maturity. The recent literature on neuroscientific findings has allowed to understand further which are the mechanisms that play the most important role in the human brain. In particular, this recent work has pointed out the importance of precocious experiences of emotional syntonization between the baby and its development partners; the quality of the experiences that such partners will be able to provide will configure no…
Electrocatalysis of neurotransmitter catecholamines by 2,4,6-triphenylpyrylium ion immobilized inside zeolite Y supercages
1999
2,4,6-Triphenylpyrylium ions entrapped inside the supercages of Y zeolite exert a remarkable catalytic effect toward the electrochemical oxidation of dopamine and norepinephrine (neurotrasmitter catecholamines) in neutral aqueous media. Domenech Carbo, Antonio, Antonio.Domenech@uv.es
GLP-2 receptor expression in excitatory and inhibitory enteric neurons and its role in mouse duodenum contractility.
2011
Background. Glucagon-like peptide 2 (GLP-2), a nutrient-responsive hormone, exerts various actions in the gastrointestinal tract that are mediated by a G-protein coupled receptor called GLP-2R. A little information is available on GLP-2R expression in enteric neurons and nothing on the interstitial cells of Cajal (ICC). Methods. We investigated presence and distribution of the GLP-2R in the mouse duodenum by immunohistochemistry and the potential motor effects of GLP-2 on the spontaneous and neurally evoked mechanical activity. Key Results. The GLP-2R was expressed by the myenteric and submucosal neurons. Labelling was also present in nerve varicosities within the circular muscular layer an…
Altered receptor binding densities in experimental antiphospholipid syndrome despite only moderately enhanced autoantibody levels and absence of beha…
2013
Abstract Experimental antiphospholipid syndrome (eAPS) in Balb/c mice causes neuropsychiatric abnormalities including hyperactivity, increased explorative behavior and cognitive deficits. Recently, we have demonstrated that these behavioral changes were linked to an upregulation of serotonergic 5-HT1A receptor binding densities in cortical and hippocampal regions while excitatory and inhibitory neurotransmitter receptors remain largely unchanged. To examine whether the observed behavioral features depend on a critical antibody concentration, mice with only moderately enhanced antiphospholipid antibodies (aPL), about 50–80% of high levels, were analyzed and compared to controls. The staircas…
Expression of inhibitory glycine receptors in postnatal rat cerebral cortex.
1993
The developmental expression of inhibitory glycine receptors was analyzed in postnatal rat cerebral cortex using the specific monoclonal antibody, MAb 4a. This antibody defines an epitope common to all known glycine receptor alpha-subunits. At birth, high levels of immunoreactivity were found, which transiently increased during the second postnatal week, but subsequently declined to low adult levels. Biochemical analysis of the MAb 4a antigen from parietal areas indicates that cortical glycine receptors correspond to the neonatal receptor isoform previously identified in spinal cord of newborn animals. Immunocytochemistry showed that, within 2 weeks after birth, MAb 4a-reactive glycine rece…
The Role of Monoamines in the Development of Cold-Induced Edema
1976
Our results show that even the experimentally induced high concentrations of exogenous 5-HT in the brain tissue during the early phase of edema formation are not able to increase the amount of fluid accumulation in the normal and injured brain tissue. The changes of the endogenous 5-HT levels in the blood and the brain tissue result in similar hemispheric water and RISA differences between the injured and uninjured half of the brain. Moreover, 5-HT concentrations elevated by 100% failed to produce detectable edema in the normal brain tissue of the rat.
Interrelation of peptidergic innervation with mast cells and ED1-positive cells in rat thymus
1991
The peptidergic innervation of rat thymus has been investigated by immunohistochemical methods, focusing on the spatial interrelationship of peptidergic nerve fibers with mast cells and macrophages in the rat. An antiserum directed against the protein gene product 9.5 (PGP 9.5) regarded as a pan-neuronal marker revealed a rich innervation, especially in the subcapsular cortex, in interlobular septa, and of the vasculature in the cortex and the corticomedullary boundary. A minor proportion of PGP 9.5-immunoreactive (ir) fibers supplied the thymic parenchyma. The main component of peptidergic innervation consisted of fibers costaining for tachykinins (TKs) and calcitonin gene-related peptide …