ArticleThe Journal of physiology2003
Nicotine is highly effective at producing desensitization of rat alpha4beta2 neuronal nicotinic receptors.
Article in The Journal of physiology, 2003. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers, 1 of them a synthesis that pooled it.
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Who cites it
58 citing papers in PubMed, 1 synthesis or guideline pooled it, 98 citations in OpenAlex.
- Neurotoxic Effects of Neonicotinoids on Mammals: What Is There beyond the Activation of Nicotinic Acetylcholine Receptors?-A Systematic Review.International journal of molecular sciences · 2021Pooled it
- Effects of cigarette smoking and abstinence on Stroop task performance.Psychopharmacology · 2007Trial
- The Effect of the Anticonvulsant Topiramate on Acetylcholine-Induced Calcium Signals is Linked to Sirt-1 Activity.The European journal of neuroscience · 2026Article
- Structural insights into the progressive recovery of α7 nicotinic acetylcholine receptor from nicotine-induced desensitization.Science advances · 2025Article
- Impacts of perinatal nicotine exposure on nicotinic acetylcholine receptor expression and glutamatergic synaptic transmission in the mouse auditory brainstem.The Journal of physiology · 2025Article
- Multiple cholinergic receptor subtypes coordinate dual modulation of acetylcholine on anterior and posterior paraventricular thalamic neurons.Journal of neurochemistry · 2024Article
- Neonicotinoid pesticides: evidence of developmental neurotoxicity from regulatory rodent studies.Frontiers in toxicology · 2024Article
- Mechanisms of Organophosphate Toxicity and the Role of Acetylcholinesterase Inhibition.Toxics · 2023Review
- Acute effects of the imidacloprid metabolite desnitro-imidacloprid on human nACh receptors relevant for neuronal signaling.Archives of toxicology · 2021Article
- Addiction-related neuroadaptations following chronic nicotine exposure.Journal of neurochemistry · 2021Review
- Functional alterations by a subgroup of neonicotinoid pesticides in human dopaminergic neurons.Archives of toxicology · 2021Article
- Article
- Nicotinic Receptors Underlying Nicotine Dependence: Evidence from Transgenic Mouse Models.Current topics in behavioral neurosciences · 2020Article
- Discovery of an intrasubunit nicotinic acetylcholine receptor-binding site for the positive allosteric modulator Br-PBTC.The Journal of biological chemistry · 2019Article
- Stoichiometry of the Heteromeric Nicotinic Receptors of the Renshaw Cell.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2018Article
- The nicotinic receptor drug sazetidine-A reduces alcohol consumption in mice without affecting concurrent nicotine consumption.Neuropharmacology · 2018Article
- Trapping of ivermectin by a pentameric ligand-gated ion channel upon open-to-closed isomerization.Scientific reports · 2017Article
- Striatal cholinergic interneurons and D2 receptor-expressing GABAergic medium spiny neurons regulate tardive dyskinesia.Experimental neurology · 2016Article
- Article
- Optogenetic activation of striatal cholinergic interneurons regulates L-dopa-induced dyskinesias.Neurobiology of disease · 2016Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
We examined desensitization by acetylcholine (ACh) and nicotine at the rat alpha4beta2 neuronal nicotinic receptor stably expressed in HEK cells. For both agonists, the decay in response due to desensitization ('onset') was best fitted by the sum of two exponentials with the fast component dominant at concentrations > 1 microM. The time constants for onset were similar for both agonists, and showed little concentration dependence over the range of 0.1-100 microM. Recovery from desensitization also showed two exponential components. In contrast to the similarity in onset, nicotine produced longer lasting desensitization, resulting from an increase in the proportion of receptors in the slowly recovering population and from an increase in the time constant for the slow recovery process. The proportion of receptors in the slowly recovering population increased as the duration of the desensitizing pulse increased. Desensitization was also induced by low concentrations of agonist, with no apparent macroscopic response. A 100 s application of 10 nM nicotine desensitized 70 % of the peak response, while 100 s of 10 nM ACh desensitized only 15 %. At higher concentrations of agonist, which result in a macroscopic response, desensitization in the absence of activation also can occur. Nicotine is a very potent and efficacious desensitizing agent at this neuronal nicotinic receptor.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.