Journal ArticleDOI
Selective allosteric enhancement of the binding and actions of acetylcholine at muscarinic receptor subtypes
Nigel J. M. Birdsall,Tim Farries,Tim Farries,Parviz Gharagozloo,Shinsaku Kobayashi,Donald Kuonen,Sebastian Lazareno,Angela Popham,Masahiko Sugimoto +8 more
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TLDR
Muscarinic agents may act only on a single muscarinic receptor subtype which is functioning sub-optimally and therefore be of use therapeutically in the early stages of Alzheimer's Disease.About:
This article is published in Life Sciences.The article was published on 1997-02-21. It has received 61 citations till now. The article focuses on the topics: Muscarinic acetylcholine receptor M2 & Muscarinic acetylcholine receptor M4.read more
Citations
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Journal Article
International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors
TL;DR: Actions of acetylcholine in the periphery are the result of activation of either the ionotropic nicotinic receptor or the metabotropic muscarinic receptor, in the mammalian central nervous system (CNS)c.
Journal ArticleDOI
Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site.
TL;DR: There are at least two distinct allosteric sites on the M(1) receptor, both of which can support positive cooperativity with acetylcholine, according to equilibrium and nonequilibrium radioligand binding studies.
Book ChapterDOI
Interference of alkaloids with neuroreceptors and ion channels
TL;DR: This review summarizes the experimental data on the molecular interactions of more than 300 alkaloids with neuroreceptors and ion channels and interprets these results under evolutionary and applied aspects, such as their exploitation as medicinal compounds or biorational pesticides for agriculture.
Journal ArticleDOI
Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
TL;DR: The results demonstrate the potential for developing allosteric enhancers of acetylcholine affinity at individual subtypes of muscarinic receptor and suggest that minor modification of a compound showing positive, neutral, or low negative cooperativity with acetyl choline may yield compounds with various patterns of cooperativity across the receptor subtypes.
Journal ArticleDOI
Allosteric interactions at muscarinic cholinoceptors
TL;DR: The muscarinic cholinoceptors represent the best‐studied examples of allosteric phenomena among the G‐protein‐coupled receptor superfamily.
References
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Journal ArticleDOI
The Cholinergic Hypothesis of Geriatric Memory Dysfunction
Raymond T. Bartus,Raymond T. Bartus,Reginald L. Dean,Bernard Beer,Bernard Beer,Arnold S. Lippa,Arnold S. Lippa +6 more
TL;DR: Biochemical, electrophysiological, and pharmacological evidence supporting a role for cholinergic dysfunction in age-related memory disturbances is critically reviewed and an attempt has been made to identify pseudoissues, resolve certain controversies, and clarify misconceptions that have occurred in the literature.
Journal ArticleDOI
Alzheimer's disease and senile dementia: loss of neurons in the basal forebrain.
Peter J. Whitehouse,Donald L. Price,Robert G. Struble,Arthur W. Clark,Joseph T. Coyle,Mahlon R. DeLong +5 more
TL;DR: Demonstration of selective degeneration of neurons of the nucleus basalis of Meynert represents the first documentation of a loss of a transmitter-specific neuronal population in a major disorder of higher cortical function and points to a critical subcortical lesion in Alzheimer's patients.
Journal ArticleDOI
GABAA Receptor Channels
TL;DR: This chapter discusses the gamma-aminobutyric acid (GABA) receptor channels, which are the most abundant inhibitory neurotransmitter in the CNS.
Journal Article
Correlation of cholinergic abnormalities with senilee plaques and mental test scores in senile dementia
TL;DR: In this paper, the authors examined brain tissue from normal (control) patients and patients with depression and dementia for activities of various cholinergic components, and these related to the degree of senile plaque formation and extent of intellectual impairment.
Journal ArticleDOI
Correlation of cholinergic abnormalities with senile plaques and mental test scores in senile dementia
TL;DR: The results suggest a close relation between changes in the cholinergic system and Alzheimer's dementia, but the precise role of the system in this disease remains to be elucidated.
Related Papers (5)
Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors.
S. Lazareno,N. J. M. Birdsall +1 more