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Choline is a Selective Agonist of α7 Nicotinic Acetylcholine Receptors in the Rat Brain Neurons
TLDR
The selective action of choline on native α7 nAChRs suggests that this naturally occurring compound may act in vivo as an endogenous ligand for these receptors.
Galantamine Is an Allosterically Potentiating Ligand of Neuronal Nicotinic but Not of Muscarinic Acetylcholine Receptors
TLDR
These studies support the previous proposal that the therapeutic action of galantamine is mainly produced by its sensitizing action on nAChRs rather than by general cholinergic enhancement due to cholinesterase inhibition.
Properties of neuronal nicotinic acetylcholine receptors: pharmacological characterization and modulation of synaptic function.
TLDR
It is an honor to receive from the American Society of Pharmacology and Experimental Therapeutics the 1996 Otto Krayer Award sponsored by Zeneca Pharmaceutics Co.
Allosteric sensitization of nicotinic receptors by galantamine, a new treatment strategy for Alzheimer’s disease
TLDR
It is found that a subgroup of cholinesterase inhibitors, including galantamine but excluding tacrine, directly interacts with nicotinic acetylcholine receptors, and these compounds, named allosterically potentiating ligands, sensitize Nicotinic receptors by increasing the probability of channel opening induced by acetyl choline and nicotinics agonists and by slowing down receptor desensitization.
Agonist responses of neuronal nicotinic acetylcholine receptors are potentiated by a novel class of allosterically acting ligands.
TLDR
The sensitizing actions of galanthamine, 5-hydroxytryptamine, and related compounds, at submicromolar concentrations, may reflect the existence of cross-talk between adjacent neuroreceptors and synapses in the central nervous system and thus suggests the formation of transiently active chemical networks in the vertebrate brain.
Memantine blocks alpha7* nicotinic acetylcholine receptors more potently than n-methyl-D-aspartate receptors in rat hippocampal neurons.
TLDR
It is suggested that blockade of alpha7(*) nAChRs by memantine could decrease its effectiveness for treatment of AD, particularly at early stages when the degrees of nA cholinergic dysfunction and of cognitive decline correlate well.
Expression of nicotinic acetylcholine receptor subunits in the cerebral cortex in Alzheimer’s disease: histotopographical correlation with amyloid plaques and hyperphosphorylated‐tau protein
TLDR
The results point to an impaired synthesis of nAChRs on the protein level as a possible cause of the cholinoceptive deficit in AD.
Memantine Blocks α7* Nicotinic Acetylcholine Receptors More Potently Than N-Methyl-D-aspartate Receptors in Rat Hippocampal Neurons
The N-methyl-d-aspartate (NMDA) receptor antagonist memantine is an approved drug for treatment of Alzheimer's disease (AD). Other such treatments are cholinesterase inhibitors and nicotinic
Diversity of nicotinic acetylcholine receptors in rat brain. V. alpha-Bungarotoxin-sensitive nicotinic receptors in olfactory bulb neurons and presynaptic modulation of glutamate release.
TLDR
The present results suggest that nicotinic synaptic transmission could play an important role in modulating the bulbar output at the glomerular level, and a presynaptic modulatory effect is one of the functions for the alpha-bungarotoxin-sensitive nAChRs in the mammalian central nervous system.
Allosteric modulation of nicotinic acetylcholine receptors as a treatment strategy for Alzheimer's disease.
TLDR
A novel class of nicotinic acetylcholine receptor ligands which, similar to the action of benzodiazepines on GABA(A) receptors, allosterically potentiate submaximal Nicotinic responses are described, which could have a preventive and corrective action on impaired but still functioningNicotinic neurotransmission.
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