Click here to close
Hello! We notice that you are using Internet Explorer, which is not supported by Xenbase and may cause the site to display incorrectly.
We suggest using a current version of Chrome,
FireFox, or Safari.
Bioorg Med Chem Lett
2005 Sep 01;1517:3874-80. doi: 10.1016/j.bmcl.2005.05.118.
Show Gene links
Show Anatomy links
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
???displayArticle.abstract???
The alpha7 nAChR subtype is of particular interest as a potential therapeutic target since it has been implicated as a mediator of both cognitive and neuroprotective activity. The rigid nicotine analog ACME and the N-cyanoborane conjugate ACME-B are selective partial agonists of rat alpha7 receptors expressed in Xenopus oocytes, with no significant activation of either alpha3beta4 or alpha4beta2 receptors. ACME-B is both more potent and efficacious than ACME. The efficacies of ACME-B and ACME are approximately 26% and 10% of the efficacy of ACh, respectively. Similar N-conjugation of S(-)nicotine with cyanoborane decreased efficacy for alpha3beta4 and alpha4beta2 receptors, as well as for alpha7 nAChR. Structural comparison of ACME with the benzylidene anabaseines, another class of previously identified alpha7-selective agonists, suggests that they share a similar structural motif that may be applicable to other alpha7-selective agonists.
Adler,
Schizophrenia, sensory gating, and nicotinic receptors.
1998, Pubmed
Adler,
Schizophrenia, sensory gating, and nicotinic receptors.
1998,
Pubmed Beers,
Structure and activity of acetylcholine.
1970,
Pubmed Boulter,
Functional expression of two neuronal nicotinic acetylcholine receptors from cDNA clones identifies a gene family.
1987,
Pubmed
,
Xenbase Clarke,
Nicotinic binding in rat brain: autoradiographic comparison of [3H]acetylcholine, [3H]nicotine, and [125I]-alpha-bungarotoxin.
1985,
Pubmed Clementi,
Neuronal nicotinic receptors, important new players in brain function.
2000,
Pubmed Costa,
A structural model of agonist binding to the alpha3beta4 neuronal nicotinic receptor.
2003,
Pubmed Elmore,
A computational study of nicotine conformations in the gas phase and in water.
2000,
Pubmed Flores,
A subtype of nicotinic cholinergic receptor in rat brain is composed of alpha 4 and beta 2 subunits and is up-regulated by chronic nicotine treatment.
1992,
Pubmed Glennon,
Musings on alpha4beta2 nicotinic acetylcholine (nACh) receptor pharmacophore models.
2004,
Pubmed Levin,
Nicotinic receptor subtypes and cognitive function.
2002,
Pubmed Meyer,
Analysis of 3-(4-hydroxy, 2-Methoxybenzylidene)anabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors.
1998,
Pubmed
,
Xenbase Meyer,
Neuroprotective and memory-related actions of novel alpha-7 nicotinic agents with different mixed agonist/antagonist properties.
1998,
Pubmed
,
Xenbase Papke,
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
2004,
Pubmed
,
Xenbase Papke,
Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonist.
2005,
Pubmed
,
Xenbase Papke,
Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis.
2002,
Pubmed
,
Xenbase Papke,
An evaluation of neuronal nicotinic acetylcholine receptor activation by quaternary nitrogen compounds indicates that choline is selective for the alpha 7 subtype.
1996,
Pubmed
,
Xenbase Papke,
The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype.
2000,
Pubmed
,
Xenbase Papke,
Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacy.
2004,
Pubmed
,
Xenbase Séguéla,
Molecular cloning, functional properties, and distribution of rat brain alpha 7: a nicotinic cation channel highly permeable to calcium.
1993,
Pubmed
,
Xenbase Stokes,
The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors.
2004,
Pubmed
,
Xenbase Whiting,
Characterization of bovine and human neuronal nicotinic acetylcholine receptors using monoclonal antibodies.
1988,
Pubmed Wu,
Mapping potential energy surfaces.
2004,
Pubmed Xu,
Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues.
2001,
Pubmed
