Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Effect of galantamine on the human alpha7 neuronal nicotinic acetylcholine receptor, the Torpedo nicotinic acetylcholine receptor and spontaneous cholinergic synaptic activity.
Texidó L, Ros E, Martín-Satué M, López S, Aleu J, Marsal J, Solsona C.
???displayArticle.abstract???
1. Various types of anticholinesterasic agents have been used to improve the daily activities of Alzheimer's disease patients. It was recently demonstrated that Galantamine, described as a molecule with anticholinesterasic properties, is also an allosteric enhancer of human alpha4beta2 neuronal nicotinic receptor activity. We explored its effect on the human alpha7 neuronal nicotinic acetylcholine receptor (nAChR) expressed in Xenopus oocytes. 2. Galantamine, at a concentration of 0.1 microM, increased the amplitude of acetylcholine (ACh)-induced ion currents in the human alpha7 nAChR expressed in Xenopus oocytes, but caused inhibition at higher concentrations. The maximum effect of galantamine, an increase of 22% in the amplitude of ACh-induced currents, was observed at a concentration of 250 microM Ach. 3. The same enhancing effect was obtained in oocytes transplanted with Torpedo nicotinic acetylcholine receptor (AChR) isolated from the electric organ, but in this case the optimal concentration of galantamine was 1 microM. In this case, the maximum effect of galantamine, an increase of 35% in the amplitude of ACh-induced currents, occurred at a concentration of 50 microM ACh. 4. Galantamine affects not only the activity of post-synaptic receptors but also the activity of nerve terminals. At a concentration of 1 microM, quantal spontaneous events, recorded in a cholinergic synapse, increased their amplitude, an effect which was independent of the anticholinesterasic activity associated with this compound. The anticholinesterasic effect was recorded in preparations treated with a galantamine concentration of 10 microM. 5. In conclusion, our results show that galantamine enhances human alpha7 neuronal nicotinic ACh receptor activity. It also enhances muscular AChRs and the size of spontaneous cholinergic synaptic events. However, only a very narrow range of galantamine concentrations can be used for enhancing effects.
Aravanis,
Single synaptic vesicles fusing transiently and successively without loss of identity.
2003, Pubmed
Aravanis,
Single synaptic vesicles fusing transiently and successively without loss of identity.
2003,
Pubmed Auld,
Alzheimer's disease and the basal forebrain cholinergic system: relations to beta-amyloid peptides, cognition, and treatment strategies.
2002,
Pubmed Bartus,
The cholinergic hypothesis of geriatric memory dysfunction.
1982,
Pubmed Brailoiu,
Inositol trisphosphate and cyclic adenosine diphosphate-ribose increase quantal transmitter release at frog motor nerve terminals: possible involvement of smooth endoplasmic reticulum.
2000,
Pubmed Brailoiu,
The vasoactive peptide urotensin II stimulates spontaneous release from frog motor nerve terminals.
2003,
Pubmed Cantí,
Tacrine and physostigmine block nicotinic receptors in Xenopus oocytes injected with Torpedo electroplaque membranes.
1998,
Pubmed
,
Xenbase Cantí,
Tacrine-induced increase in the release of spontaneous high quantal content events in Torpedo electric organ.
1994,
Pubmed Coyle,
Alzheimer's disease: a disorder of cortical cholinergic innervation.
1983,
Pubmed Dale,
Clinical experience of galantamine in dementia: a series of case reports.
2003,
Pubmed Davies,
Selective loss of central cholinergic neurons in Alzheimer's disease.
1976,
Pubmed Dumont,
Oogenesis in Xenopus laevis (Daudin). I. Stages of oocyte development in laboratory maintained animals.
1972,
Pubmed
,
Xenbase Dunant,
Quantal release of acetylcholine evoked by focal depolarization at the Torpedo nerve-electroplaque junction.
1986,
Pubmed Gandhi,
Three modes of synaptic vesicular recycling revealed by single-vesicle imaging.
2003,
Pubmed Giacobini,
Cholinergic function and Alzheimer's disease.
2003,
Pubmed Kraliz,
Selective blockade of the delayed rectifier potassium current by tacrine in Drosophila.
1997,
Pubmed Li,
Bis(7)-tacrine, a novel dimeric AChE inhibitor, is a potent GABA(A) receptor antagonist.
1999,
Pubmed López,
Solid-phase extraction and reversed-phase high-performance liquid chromatography of the five major alkaloids in Narcissus confusus.
2002,
Pubmed Maelicke,
Allosteric modulation of Torpedo nicotinic acetylcholine receptor ion channel activity by noncompetitive agonists.
1997,
Pubmed Maelicke,
Allosteric sensitization of nicotinic receptors by galantamine, a new treatment strategy for Alzheimer's disease.
2001,
Pubmed Marsal,
Incorporation of acetylcholine receptors and Cl- channels in Xenopus oocytes injected with Torpedo electroplaque membranes.
1995,
Pubmed
,
Xenbase Miledi,
Effects of defolliculation on membrane current responses of Xenopus oocytes.
1989,
Pubmed
,
Xenbase Miwa,
lynx1, an endogenous toxin-like modulator of nicotinic acetylcholine receptors in the mammalian CNS.
1999,
Pubmed
,
Xenbase Mulle,
Potentiation of nicotinic receptor response by external calcium in rat central neurons.
1992,
Pubmed Muller,
Spontaneous quantal and subquantal transmitter release at the Torpedo nerve-electroplaque junction.
1987,
Pubmed Papke,
Activation and inhibition of rat neuronal nicotinic receptors by ABT-418.
1997,
Pubmed
,
Xenbase Pereira,
Unconventional ligands and modulators of nicotinic receptors.
2002,
Pubmed Pereira,
Identification and functional characterization of a new agonist site on nicotinic acetylcholine receptors of cultured hippocampal neurons.
1993,
Pubmed Pereira,
Physostigmine and galanthamine: probes for a novel binding site on the alpha 4 beta 2 subtype of neuronal nicotinic acetylcholine receptors stably expressed in fibroblast cells.
1994,
Pubmed Ros,
Effects of bis(7)-tacrine on spontaneous synaptic activity and on the nicotinic ACh receptor of Torpedo electric organ.
2001,
Pubmed
,
Xenbase Ros,
Effects of CI-1002 and CI-1017 on spontaneous synaptic activity and on the nicotinic acetylcholine receptor of Torpedo electric organ.
2000,
Pubmed
,
Xenbase Ros,
The pharmacology of novel acetylcholinesterase inhibitors, (+/-)-huprines Y and X, on the Torpedo electric organ.
2001,
Pubmed
,
Xenbase Samochocki,
Galantamine is an allosterically potentiating ligand of neuronal nicotinic but not of muscarinic acetylcholine receptors.
2003,
Pubmed Santos,
The nicotinic allosteric potentiating ligand galantamine facilitates synaptic transmission in the mammalian central nervous system.
2002,
Pubmed Sharp,
Effects of galantamine, a nicotinic allosteric potentiating ligand, on nicotine-induced catecholamine release in hippocampus and nucleus accumbens of rats.
2004,
Pubmed Shaw,
The reversible cholinesterase inhibitor physostigmine has channel-blocking and agonist effects on the acetylcholine receptor-ion channel complex.
1985,
Pubmed Thomsen,
Inhibition of acetylcholinesterase activity in human brain tissue and erythrocytes by galanthamine, physostigmine and tacrine.
1991,
Pubmed Van der Kloot,
The regulation of quantal size.
1991,
Pubmed Vernino,
Calcium modulation and high calcium permeability of neuronal nicotinic acetylcholine receptors.
1992,
Pubmed
,
Xenbase Woodruff-Pak,
Galantamine: effect on nicotinic receptor binding, acetylcholinesterase inhibition, and learning.
2001,
Pubmed Zhang,
Cholinergic drugs for Alzheimer's disease enhance in vitro dopamine release.
2004,
Pubmed
