Search results for "nicotinic agonist"
showing 10 items of 118 documents
Chapter 27: Peptidergic and cholinergic receptors on cultured astrocytes of different regions of the rat CNS
1992
Publisher Summary This chapter discusses whether astrocytes possess peptidergic and cholinergic receptors. There is strong evidence that in addition to neurons, astrocytes also express receptors for neurotransmitters and neuromodulators. The investigations were carried out in explant cultures of the spinal cord, brain-stem, cerebellum, and neocortex of fetal and newborn rats. By the means of autoradiography, it was demonstrated that astrocytes possess binding sites for the vasoactive peptides 3 H-Ang II, 125 I- VIP, 125 I-ET-l, ET-3, and 125 I-AVP. These findings are consistent with electrophysiological studies demonstrating that Ang II, ET, and AVP cause a depolarization of the glial membr…
Corrigendum to: α-Conotoxins EpI and AuIB switch subtype selectivity and activity in native versus recombinant nicotinic acetylcholine receptors (FEB…
2003
Corrigendum to: K-Conotoxins EpI and AuIB switch subtype selectivity and activity in native versus recombinant nicotinic acetylcholine receptors (FEBS 27779) [FEBS Letters 554 (2003) 219^223]C Annette Nickea;1, Marek Samochockib, Marion L. Loughnana, Paramjit S. Bansala, Alfred Maelickeb, Richard J. Lewisa; aInstitute for Molecular Bioscience, University of Queensland, Brisbane, Qld. 4072, Australia bInstitute for Physiological Chemistry and Pathobiochemistry, University of Mainz, D-55099 Mainz, Germany First published online 24 December 2003
Synthesis and in vitro evaluation of galanthamine derivatives for examination of nicotinic acetylcholine receptor system
2001
ISunmrary: The syntheses and radioactive labeling of several galanthamine derivatives, 6-O-demethyl-6-O-fluoroethylgalanthamine, 10-N-demethyl-lO-Nfluoroethylgalanthamine and N-methylgalanthaminium are reported. First ill vitro evaluations were carried out to determine their properties as allosterically potentiating ligands of nicotinic receptors. N-methylgalanthaminium was found to be a promising candidate for further investigations. The most commonly applied therapeutic approach to balance nicotinic cholinergic deficits in Alzheimer’s disease (AD) patients is the administration of acetylcholinesterase inhibitors (AChE-I) although they have been proven to be of limited therapeutic value [ …
Allosteric modulation of nicotinic acetylcholine receptors as a treatment strategy for Alzheimer's disease
2000
The basic symptoms of Alzheimer's dementia, i.e., a loss in cognitive function, are due to impaired nicotinic cholinergic neurotransmission. To compensate for this impairment by drug treatment, blockers of the acetylcholine-degrading enzyme acetylcholinesterase are applied, even though this approach obviously is prone to many side-effects, including those of muscarinic nature. We have recently described a novel class of nicotinic acetylcholine receptor ligands which, similar to the action of benzodiazepines on GABA(A) receptors, allosterically potentiate submaximal nicotinic responses. The sensitizing effect is a consequence of facilitated channel opening in the presence of allosterically p…
Immunohistochemistry of cholinergic receptors.
1992
Acetylcholine and its receptors are involved in a variety of important signal transduction processes. As shown here paradigmatically for the human neuromuscular junction and the cerebral cortex, acetylcholine receptors can be visualized immunohistochemically at the cellular and subcellular level under physiological and pathological conditions. At normal motor endplates nicotinic cholinoceptors are localized at the surface of the postsynaptic junctional folds. In myasthenic syndromes investigation of muscle biopsies enables the diagnosis of receptor deficiencies at the ultrastructural level. In normal cerebral cortex pyramidal neurons are equipped with both nicotinic and muscarinic acetylcho…
Cellular distribution in the rat telencephalon of mRNAs encoding for the alpha 3 and alpha 4 subunits of the nicotinic acetylcholine receptor.
1995
Pharmacological and electrophysiological studies provide evidence for the involvement of different nicotinic acetylcholine receptor isoforms in rat neocortical and hippocampal signal transduction. Yet, rather little is known on the cellular localization of these isoforms. With the availability of isoform specific nucleic acid probes and sensitive non-isotopic detection systems, nicotinic receptors can be studied on the mRNA level in individual neurons. In this way, we have paradigmatically studied the distribution of the alpha 3 and alpha 4 isoform mRNAs of the nicotinic receptor in the rat telencephalon. In the cerebral cortex, alpha 3 transcripts were mainly located in pyramidal neurons o…
Expression of the Acetylcholine Receptor α-Subunit Gene is Associated with Paraneoplastic Myasthenia Gravis in Mixed Thymoma
2000
Myasthenia gravis (MG) is an autoimmune disease caused by autoantibodies against the acetylcholine receptor (AChR) at the neuromuscular junction [1]. The muscular AChR has been extensively characterized [2], but the etiology of MG is still obscure. Whether the muscular AChR or another (auto)antigen plays a role during the initiation of MG is unknown [3]. The muscular AChR is a pentameric ion channel composed of four different subunits. The α-subunit contains the acetylcholine binding site and the main epitopes recognized by MG autoantibodies [2]. The human muscle AChR α-subunit exists as two isoforms, P3A- and P3A+ [4]. This is a result of alternative splicing of the P3A exon located betwee…
Modulatory control by non-competitive agonists of nicotinic cholinergic neurotransmission in the central nervous system
1995
Abstract Several exogenous and endogenous compounds have been discovered that act on nicotinic acetylcholine receptors as non-competitive agonists (NCA) of low efficacy, and probably also as allosteric regulators of the receptor's sensitivity to acetylcholine. Nicotinic NCAs may be viewed as another facet in the increasingly complex picture of vertebrate brain organization, i.e. they may be part of a higher level ‘chemical’ network that overlays the neuronal network of the CNS. Furthermore, exogenous NCAs may provide a new therapeutic approach to Alzheimer's dementia.
Expression and function of the non-neuronal cholinergic system in endothelial cells
2003
Increasing evidence has shown the expression of the non-neuronal cholinergic system in endothelial cells. In the present experiments the expression of choline acetyltransferase (ChAT) was investigated in human endothelial cells by anti-ChAT immunohistochemistry and anti-ChAT immunofluorescence. Positive ChAT immunoreactivity was found in cultures of human umbilical endothelial cells (HUVEC) and a human angiosarcoma cell line (HAEND). In HUVEC and HAEND choline acetyltransferase activity and small amounts of acetylcholine were also detected. Positive ChAT-immunoreactivity was demonstrated in situ in endothelial cells of the human umbilical cord. In addition, in experiments with confocal lase…
Colocalization but differential regulation of neuronal NO synthase and nicotinic acetylcholine receptor in C2C12 myotubes.
2003
In mammalian skeletal muscle, neuronal-type nitric oxide synthase (nNOS) is found to be enriched at neuromuscular endplates. Here we demonstrate the colocalization of the nicotinic acetylcholine receptor (nAChR, stained with α-bungarotoxin) and nNOS (stained with a specific antibody) in murine C2C12myotubes. However, coimmunoprecipitation experiments demonstrated no evidence for a direct protein-protein association between the nAChR and nNOS in C2C12myotubes. An antibody to the α1-subunit of the nAChR did not coprecipitate nNOS, and an nNOS-specific antibody did not precipitate the α1-subunit of the nAChR. Treatment of mice with bacterial LPS downregulated the expression of nNOS in skeletal…