ArticleBiochemical pharmacology2010
86Rb+ efflux mediated by alpha4beta2*-nicotinic acetylcholine receptors with high and low-sensitivity to stimulation by acetylcholine display similar agonist-induced desensitization.
Article in Biochemical pharmacology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed, 33 citations in OpenAlex.
- Population Pharmacodynamic Models of Risperidone on PANSS Total Scores and Prolactin Levels in Schizophrenia.Pharmaceuticals (Basel, Switzerland) · 2024Article
- Acute effects of the imidacloprid metabolite desnitro-imidacloprid on human nACh receptors relevant for neuronal signaling.Archives of toxicology · 2021Article
- Functional alterations by a subgroup of neonicotinoid pesticides in human dopaminergic neurons.Archives of toxicology · 2021Article
- Nicotinic Acetylcholine Receptor Accessory Subunits Determine the Activity Profile of Epibatidine Derivatives.Molecular pharmacology · 2020Article
- The α5 Nicotinic Acetylcholine Receptor Subunit Differentially Modulates α4β2Frontiers in synaptic neuroscience · 2020Review
- Developmental nicotine exposure precipitates multigenerational maternal transmission of nicotine preference and ADHD-like behavioral, rhythmometric, neuropharmacological, and epigenetic anomalies in adolescent mice.Neuropharmacology · 2019Article
- The interaction of the Chrna5 D398N variant with developmental nicotine exposure.Genes, brain, and behavior · 2018Article
- The fifth subunit of the (α4β2)British journal of pharmacology · 2018Article
- Manipulation of Subunit Stoichiometry in Heteromeric Membrane Proteins.Structure (London, England : 1993) · 2016Article
- Pharmacologically distinct nicotinic acetylcholine receptors drive efferent-mediated excitation in calyx-bearing vestibular afferents.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2015Article
- Non-equivalent ligand selectivity of agonist sites in (α4β2)2α4 nicotinic acetylcholine receptors: a key determinant of agonist efficacy.The Journal of biological chemistry · 2014Article
- Nicotinic acetylcholine receptors in attention circuitry: the role of layer VI neurons of prefrontal cortex.Cellular and molecular life sciences : CMLS · 2014Review
- Rare human nicotinic acetylcholine receptor α4 subunit (CHRNA4) variants affect expression and function of high-affinity nicotinic acetylcholine receptors.The Journal of pharmacology and experimental therapeutics · 2014Article
- The unique α4+/-α4 agonist binding site in (α4)3(β2)2 subtype nicotinic acetylcholine receptors permits differential agonist desensitization pharmacology versus the (α4)2(β2)3 subtype.The Journal of pharmacology and experimental therapeutics · 2014Article
- Selective potentiation of (α4)3(β2)2 nicotinic acetylcholine receptors augments amplitudes of prefrontal acetylcholine- and nicotine-evoked glutamatergic transients in rats.Biochemical pharmacology · 2013Article
- The additional ACh binding site at the α4(+)/α4(-) interface of the (α4β2)2α4 nicotinic ACh receptor contributes to desensitization.British journal of pharmacology · 2013Article
- Unravelling the mechanism of action of NS9283, a positive allosteric modulator of (α4)3(β2)2 nicotinic ACh receptors.British journal of pharmacology · 2013Article
- CC4, a dimer of cytisine, is a selective partial agonist at α4β2/α6β2 nAChR with improved selectivity for tobacco smoking cessation.British journal of pharmacology · 2013Article
- Mice expressing the ADNFLE valine 287 leucine mutation of the Β2 nicotinic acetylcholine receptor subunit display increased sensitivity to acute nicotine administration and altered presynaptic nicotinic receptor function.Pharmacology, biochemistry, and behavior · 2013Article
- Glutamatergic and GABAergic metabolism in mouse brain under chronic nicotine exposure: implications for addiction.PloS one · 2012Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
The nicotinic acetylcholine receptors (nAChR) assembled from alpha4 and beta2 subunits are the most densely expressed subtype in the brain. Concentration-effect curves for agonist activation of alpha4beta2*-nAChR are biphasic. This biphasic agonist sensitivity is ascribed to differences in subunit stoichiometry. The studies described here evaluated desensitization elicited by low concentrations of epibatidine, nicotine, cytisine or methylcarbachol of brain alpha4beta2-nAChR function measured with acetylcholine-stimulated (86)Rb(+) efflux from mouse thalamic synaptosomes. Each agonist elicited concentration-dependent desensitization. The agonists differed in potency. However, IC(50) values for each agonist for desensitization of (86)Rb(+) efflux both with high (EC(50) approximately 3 microM) and low (EC(50) approximately 150 microM) acetylcholine sensitivity were not significantly different. Concentrations required to elicit desensitization were higher that their respective K(D) values for receptor binding. Even though the two components of alpha4beta2*-nAChR-mediated (86)Rb(+) efflux from mouse brain differ markedly in EC(50) values for agonist activation, they are equally sensitive to desensitization by exposure to low agonist concentrations. Mice were also chronically treated with nicotine by continuous infusion of 0, 0.5 or 4.0mg/kg/h and desensitization induced by nicotine was evaluated. Consistent with previous results, chronic nicotine treatment increased the density of epibatidine binding sites. Acute exposure to nicotine also elicited concentration-dependent desensitization of both high-sensitivity and low-sensitivity acetylcholine-stimulated (86)Rb(+) efflux from cortical and thalamic synaptosomes. Although chronic nicotine treatment reduced maximal (86)Rb(+) efflux from thalamus, IC(50) values in both brain regions were unaffected by chronic nicotine treatment.
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