5,8-Disubstituted indolizidines: A new class of noncompetitive blockers for nicotinic receptor-channels

1991 ◽  
Vol 16 (11) ◽  
pp. 1213-1218 ◽  
Author(s):  
John W. Daly ◽  
Yukio Nishizawa ◽  
William L. Padgett ◽  
Takashi Tokuyama ◽  
Adrian L. Smith ◽  
...  
Keyword(s):  
Nicotinic Receptor ◽  
New Class ◽  
Nicotinic Receptor Channels ◽  
Noncompetitive Blockers

scholarly journals ω-agatoxin IVA blocks nicotinic receptor channels in bovine chromaffin cells

FEBS Letters ◽  
1995 ◽  
Vol 362 (1) ◽  
pp. 15-18 ◽  
Author(s):  
Ricardo Granja ◽  
JoséM Fernández-Fernández ◽  
Victor Izaguirre ◽  
Carmen González-García ◽  
Valentin Ceña
Keyword(s):  
Nicotinic Receptor ◽  
Chromaffin Cells ◽  
Bovine Chromaffin Cells ◽  
Nicotinic Receptor Channels

Block of recombinant nicotinic receptor channels by IgG from myasthenic patients

2002 ◽  
Vol 25 (3) ◽  
pp. 433-437 ◽  
Author(s):  
Klaus Krampfl ◽  
Reinhard Dengler ◽  
Johannes Bufler
Keyword(s):  
Nicotinic Receptor ◽  
Nicotinic Receptor Channels

Varenicline: Implications for the Field

2007 ◽  
Vol 2 (S1) ◽  
pp. 8-11 ◽  
Author(s):  
Alex Bobak
Keyword(s):  
Smoking Cessation ◽  
Nicotinic Receptor ◽  
Partial Agonist ◽  
Nicotine Patch ◽  
Clinical Excellence ◽  
Common Side Effect ◽  
Safety And Efficacy ◽  
New Class ◽  
Good Safety Profile ◽  
Final Guidance

AbstractVarenicline tartrate (Champix) is the first in a new class of therapy for smoking cessation and has been available on NHS prescription since December 2006. It has received approval from The National Institute for Health and Clinical Excellence (NICE) and the Scottish Medicines Consortium and NICE final guidance was issued in July 2007. Varenicline is a partial agonist of the nicotinic receptor (·4, 2 subtype) and also prevents nicotine from binding to it. Studies comparing safety and efficacy with bupropion (Zyban) have been favourable and efficacy with varenicline has been shown to be greater than that with bupropion. A study comparing the nicotine patch is due for publication this year. Varenicline has a good safety profile with nausea being the most common side effect in about a third of those who take it. Despite the treatment's advantages there have been numerous issues which have affected its use. These include funding and administrative issues and this paper looks at ways of overcoming those barriers to prescribing what is a valuable addition to the range of treatments on offer to smokes who want to stop.

Nicotinic receptor-elicited sodium flux in rat pheochromocytoma PC12 cells: Effects of agonists, antagonists, and noncompetitive blockers

1991 ◽  
Vol 16 (4) ◽  
pp. 489-500 ◽  
Author(s):  
John W. Daly ◽  
Yukio Nishizawa ◽  
Michael W. Edwards ◽  
James A. Waters ◽  
Robert S. Aronstam
Keyword(s):  
Pc12 Cells ◽  
Nicotinic Receptor ◽  
Sodium Flux ◽  
Pheochromocytoma Pc12 ◽  
Pheochromocytoma Pc12 Cells ◽  
Noncompetitive Blockers

scholarly journals Pharmacological receptors of nematoda as target points for action of antiparasitic drugs

2010 ◽  
Vol 64 (3-4) ◽  
pp. 253-264
Author(s):  
Sasa Trailovic ◽  
Sasa Ivanovic ◽  
Jelena Trailovic-Nedeljkovic ◽  
Alan Robertson
Keyword(s):  
Veterinary Medicine ◽  
Nicotinic Receptor ◽  
Cholinergic Receptors ◽  
Parasitic Nematodes ◽  
Somatic Muscle ◽  
Nicotinic Acetylcholine ◽  
New Class ◽  
Site Of Action ◽  
Antiparasitic Drugs ◽  
Sites Of Action

Cholinergic receptors of parasitic nematodes are one of the most important possible sites of action of antiparasitic drugs. This paper presents some of our own results of electrophysiological and pharamcological examinations of nicotinic and muscarinic receptors of nematodes, as well as data from literature on a new class of anthelmintics that act precisely on cholinergic receptors. The nicotinic acetylcholine receptor (nAChR) is located on somatic muscle cells of nematodes and it is responsible for the coordination of parasite movement. Cholinomimetic anthelmintics act on this receptor, as well as acetylcholine, an endogenic neurotransmitter, but they are not sensitive to enzyme acetylcholineesterase which dissolves acetylcholine. As opposed to the nicotinic receptor of vertebra, whose structure has been examined thoroughly, the stoichiometry of the nicotinic receptor of nematodes is not completely known. However, on the grounds of knowledge acquired so far, a model has been constructed recently of the potential composition of a type of nematodes nicotinic receptor, as the site of action of anthelmintics. Based on earlier investigations, it is supposed that a conventional muscarinic receptor exists in nematodes as well, so that it can also be a new pharamocological target for the development of antinematode drugs. The latest class of synthesized anthelmintics, named aminoacetonitriles (AAD), act via the nicotinic receptor. Monepantel is the first drug from the AAD group as a most significant candidate for registration in veterinary medicine. Even though several groups of cholinomimetic anthelmintics (imiodazothiazoles, tetrahydropyrimidines, organophosphat anthelmintics) have been in use in veterinary practice for many years now, it is evident that cholinergic receptors of nematodes still present an attractive place in the examinations and development of new antinematode drugs. .

Activation of Single Nicotinic Receptor Channels from Caenorhabditis elegans Muscle

2007 ◽  
Vol 71 (5) ◽  
pp. 1407-1415 ◽  
Author(s):  
Diego Rayes ◽  
Marina Flamini ◽  
Guillermina Hernando ◽  
Cecilia Bouzat
Keyword(s):  
Caenorhabditis Elegans ◽  
Nicotinic Receptor ◽  
Nicotinic Receptor Channels

scholarly journals α-Selenoconotoxins, a New Class of Potent α7Neuronal Nicotinic Receptor Antagonists

2006 ◽  
Vol 281 (20) ◽  
pp. 14136-14143 ◽  
Author(s):  
Christopher J. Armishaw ◽  
Norelle L. Daly ◽  
Simon T. Nevin ◽  
David J. Adams ◽  
David J. Craik ◽  
...  
Keyword(s):  
Nicotinic Receptor ◽  
Receptor Antagonists ◽  
New Class
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