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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
.
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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
