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.
ACS Chem Neurosci
2014 Aug 20;58:683-9. doi: 10.1021/cn5000748.
Show Gene links
Show Anatomy links
Effect of triazine derivatives on neuronal nicotinic receptors.
Vázquez-Romero A
,
Criado M
,
Messeguer A
,
Vidal-Mosquera M
,
Mulet J
,
Sala F
,
Sala S
.
???displayArticle.abstract???
We have characterized the effect of triazine derivatives on neuronal nicotinic receptors expressed in Xenopus oocytes. All triazines investigated inhibit the current of α7 and α3β4 neuronal nicotinic receptors elicited by acetylcholine. The effect is concentration dependent, reversible, and noncompetitive. In contrast, some derivatives have a dual effect on α4β2 receptors, by potentiating the currents at intermediate concentration and causing inhibition at higher concentrations. Triazine derivatives also affect the macroscopic kinetics of the heteromeric receptors α3β4 and α4β2 accelerating the rise and decay time course of the currents, but have no significant effect on the kinetics of homomeric α7 receptors. Two simple kinetic models are presented. The first reproduces the effects of different concentrations of triazines both on the peak currents and on the macroscopic kinetics of α7 with a simple inhibitory result. The second model describes the behavior of α4β2 receptors involving a more complex dual action.
Colquhoun,
Fast events in single-channel currents activated by acetylcholine and its analogues at the frog muscle end-plate.
1985, Pubmed
Colquhoun,
Fast events in single-channel currents activated by acetylcholine and its analogues at the frog muscle end-plate.
1985,
Pubmed
Edelstein,
A kinetic mechanism for nicotinic acetylcholine receptors based on multiple allosteric transitions.
1996,
Pubmed
García-Guzmán,
Role of two acetylcholine receptor subunit domains in homomer formation and intersubunit recognition, as revealed by alpha 3 and alpha 7 subunit chimeras.
1994,
Pubmed
,
Xenbase
Hurst,
Nicotinic acetylcholine receptors: from basic science to therapeutics.
2013,
Pubmed
Krashia,
Human α3β4 neuronal nicotinic receptors show different stoichiometry if they are expressed in Xenopus oocytes or mammalian HEK293 cells.
2010,
Pubmed
,
Xenbase
Krieg,
Functional messenger RNAs are produced by SP6 in vitro transcription of cloned cDNAs.
1984,
Pubmed
,
Xenbase
Milescu,
Maximum likelihood estimation of ion channel kinetics from macroscopic currents.
2005,
Pubmed
Moroni,
alpha4beta2 nicotinic receptors with high and low acetylcholine sensitivity: pharmacology, stoichiometry, and sensitivity to long-term exposure to nicotine.
2006,
Pubmed
,
Xenbase
Moroni,
Non-agonist-binding subunit interfaces confer distinct functional signatures to the alternate stoichiometries of the alpha4beta2 nicotinic receptor: an alpha4-alpha4 interface is required for Zn2+ potentiation.
2008,
Pubmed
,
Xenbase
Pandya,
Allosteric modulators of the α4β2 subtype of neuronal nicotinic acetylcholine receptors.
2011,
Pubmed
Paterson,
Neuronal nicotinic receptors in the human brain.
2000,
Pubmed
,
Xenbase
Pesti,
Kinetic properties and open probability of α7 nicotinic acetylcholine receptors.
2014,
Pubmed
Sala,
Effects of benzothiazepines on human neuronal nicotinic receptors expressed in Xenopus oocytes.
2002,
Pubmed
,
Xenbase
Szabo,
Mode of action of the positive modulator PNU-120596 on α7 nicotinic acetylcholine receptors.
2014,
Pubmed
Vallés,
Lamotrigine is an open-channel blocker of the nicotinic acetylcholine receptor.
2007,
Pubmed
Vallés,
A novel agonist effect on the nicotinic acetylcholine receptor exerted by the anticonvulsive drug Lamotrigine.
2008,
Pubmed
Vidal-Mosquera,
Triazine-based vanilloid 1 receptor open channel blockers: design, synthesis, evaluation, and SAR analysis.
2011,
Pubmed
,
Xenbase
Williams,
Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.
2011,
Pubmed
Zheng,
The anticonvulsive drug lamotrigine blocks neuronal {alpha}4{beta}2 nicotinic acetylcholine receptors.
2010,
Pubmed
