Journal ArticleDOI
Neuronal Nicotinic Acetylcholine Receptors as Targets for Drug Discovery
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This article is published in Journal of Medicinal Chemistry.The article was published on 1997-12-19. It has received 504 citations till now. The article focuses on the topics: Nicotinic agonist & Nicotinic Antagonist.read more
Citations
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Journal ArticleDOI
Metabolism and Disposition Kinetics of Nicotine
TL;DR: Current knowledge about the metabolism and disposition kinetics of nicotine, some other naturally occurring tobacco alkaloids, and nicotine analogs that are under development as potential therapeutic agents are reviewed.
Journal ArticleDOI
NEONICOTINOID INSECTICIDE TOXICOLOGY: Mechanisms of Selective Action
Motohiro Tomizawa,John E. Casida +1 more
TL;DR: The neonicotinoids have outstanding potency and systemic action for crop protection against piercing-sucking pests, and they are highly effective for flea control on cats and dogs.
Journal ArticleDOI
Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation
Jotham Wadsworth Coe,Paige Roanne Palmer Brooks,Michael G. Vetelino,Michael C. Wirtz,Eric P. Arnold,Huang Jianhua,Steven B. Sands,Thomas I. Davis,Lorraine A. Lebel,Carol B. Fox,Alka Shrikhande,James Heym,Eric Schaeffer,Hans Rollema,Yi Lu,Robert S. Mansbach,Leslie K. Chambers,Charles C. Rovetti,David W. Schulz,and F. David Tingley,Brian T. O’Neill +20 more
TL;DR: Varenicline displays high α4β2 nAChR affinity and the desired in vivo dopaminergic profile and provides relief from the craving and withdrawal syndrome that accompanies cessation attempts.
Patent
Inhibition of inflammatory cytokine production by cholinergic agonists and vagus nerve stimulation
TL;DR: In this article, a method of inhibiting the release of a proinflammatory cytokine in a cell is disclosed, which comprises treating the cell with a cholinergic agonist, which is useful in patients at risk for, or suffering from, a condition mediated by an inflammatory cytokine cascade, for example endotoxic shock.
Journal Article
Neuronal nicotinic acetylcholine receptors as novel drug targets.
G K Lloyd,M Williams +1 more
TL;DR: The plant alkaloid, nicotine, is a commonly used psychoactive drug that is orally self-administered via the chewing or combustion of tobacco products, the latter typically via cigarette use.
References
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Journal ArticleDOI
Atomic structure of acetylcholinesterase from Torpedo californica: a prototypic acetylcholine-binding protein
Joel L. Sussman,Michal Harel,Felix Frolow,Christian Oefner,Adrian Goldman,Lilly Toker,Israel Silman +6 more
TL;DR: Modeling of acetylcholine binding to the enzyme suggests that the quaternary ammonium ion is bound not to a negatively charged "anionic" site, but rather to some of the 14 aromatic residues that line the gorge.
Journal ArticleDOI
Cation-π Interactions in Chemistry and Biology: A New View of Benzene, Phe, Tyr, and Trp
TL;DR: A great deal of direct and circumstantial evidence indicates that cation-π interactions are important in a variety of proteins that bind cationic ligands or substrates.
Journal ArticleDOI
Molecular cloning, functional properties, and distribution of rat brain alpha 7: a nicotinic cation channel highly permeable to calcium
TL;DR: The results imply that alpha 7-containing receptors may play a role in activating calcium-dependent mechanisms in specific neuronal populations of the adult rat limbic system.
Journal ArticleDOI
Changing subunit composition of heteromeric NMDA receptors during development of rat cortex
TL;DR: Direct evidence is presented that NMDA receptors exist in rat neocortex as heteromeric complexes of considerable heterogeneity, some containing both NR2A and NR2B subunits.
Journal ArticleDOI
Presynaptic nicotinic ACh receptors.
TL;DR: Nicotinic ACh receptors in the CNS are composed of a diverse array of subunits and have a range of pharmacological properties but despite the fact that they are ligand-gated cation channels, their physiological functions have not been determined.
Related Papers (5)
International Union of Pharmacology. XX. Current Status of the Nomenclature for Nicotinic Acetylcholine Receptors and Their Subunits
Ronald J. Lukas,Jean-Pierre Changeux,N. Le Novere,Edson X. Albuquerque,David J.K. Balfour,Darwin K. Berg,D. Bertrand,Vincent A. Chiappinelli,P. B. S. Clarke,Allan C. Collins,J. A. Dani,Sharon R. Grady,Kenneth J. Kellar,Jon Lindstrom,Michael J. Marks,Maryka Quik,Palmer Taylor,Susan Wonnacott +17 more