ArticleThe Journal of pharmacology and experimental therapeutics2005
Modulation of human 5-hydroxytryptamine type 3AB receptors by volatile anesthetics and n-alcohols.
Article in The Journal of pharmacology and experimental therapeutics, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 53 citations in OpenAlex.
- The incidences of nausea and vomiting after general anesthesia with remimazolam versus sevoflurane: a prospective randomized controlled trial.Korean journal of anesthesiology · 2024Trial
- Relevance of Cortical and Hippocampal Interneuron Functional Diversity to General Anesthetic Mechanisms: A Narrative Review.Frontiers in synaptic neuroscience · 2021Review
- Update on the Mechanism and Treatment of Sevoflurane-Induced Postoperative Cognitive Dysfunction.Frontiers in aging neuroscience · 2021Review
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Allosteric potentiation of a ligand-gated ion channel is mediated by access to a deep membrane-facing cavity.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Structural Basis of Alcohol Inhibition of the Pentameric Ligand-Gated Ion Channel ELIC.Structure (London, England : 1993) · 2017Article
- Improved scFv Anti-LOX-1 Binding Activity by Fusion with LOX-1-Binding Peptides.BioMed research international · 2017Article
- Novel mechanism of modulation at a ligand-gated ion channel; action of 5-Cl-indole at the 5-HTBritish journal of pharmacology · 2016Article
- Differential effects of volatile anesthetics on leukocyte integrin macrophage-1 antigen.Journal of immunotoxicology · 2016Article
- Seeking structural specificity: direct modulation of pentameric ligand-gated ion channels by alcohols and general anesthetics.Pharmacological reviews · 2014Review
- Discriminating between 5-HT₃A and 5-HT₃AB receptors.British journal of pharmacology · 2013Review
- Novel activation of voltage-gated K(+) channels by sevoflurane.The Journal of biological chemistry · 2012Article
- Functional genetic variants that increase synaptic serotonin and 5-HT3 receptor sensitivity predict alcohol and drug dependence.Molecular psychiatry · 2011Article
- Therapeutics of 5-HT3 receptor antagonists: current uses and future directions.Pharmacology & therapeutics · 2011Review
- Allosteric modulation of the 5-HT(3) receptor.Current opinion in pharmacology · 2011Review
- Sevoflurane binds and allosterically blocks integrin lymphocyte function-associated antigen-1.Anesthesiology · 2010Article
- Ethanol stabilizes the open state of single 5-hydroxytryptamine(3A)(QDA) receptors.The Journal of pharmacology and experimental therapeutics · 2010Article
- Acute alcohol action and desensitization of ligand-gated ion channels.Pharmacological reviews · 2009Review
- HTR3B is associated with alcoholism with antisocial behavior and alpha EEG power--an intermediate phenotype for alcoholism and co-morbid behaviors.Alcohol (Fayetteville, N.Y.) · 2009Article
- Inhibition of human 5-HT(3A) and 5-HT(3AB) receptors by etomidate, propofol and pentobarbital.European journal of pharmacology · 2007Article
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Functional 5-hydroxytryptamine type 3 (5-HT3) receptors can be formed by 5-HT3A subunits alone or in combination with the 5-HT3B subunit, but only the 5-HT3A receptor has been previously studied with respect to the modulation by volatile anesthetics and n-alcohols. Using two-electrode voltage-clamp, we show for the first time the modulation of heteromeric human (h)5-HT3AB receptors, expressed in Xenopus oocytes, by a series of n-alcohols and halogenated volatile anesthetics. At twice their anesthetic concentration, compounds having a molecular volume of less than 110 A3 enhanced submaximal 5-HT-evoked current. Compounds larger than 110 A3 inhibited submaximal 5-HT-evoked current. In experiments examining 5-HT concentration-response relationships, chloroform and butanol caused a slight decrease in the 5-HT EC50. Sevoflurane and octanol inhibited 5-HT-evoked current at all 5-HT concentrations tested but had no effect upon the 5-HT EC50. Compared with previous data on homomeric h5-HT3A receptors, the presence of the h5-HT3B subunit reduces the enhancement of h5-HT3 receptors by smaller halogenated volatile anesthetics and n-alcohols. In summary, these results suggest that heteromeric h5-HT3AB receptors are modulated by halogenated volatile anesthetics at clinically relevant concentrations, in addition to n-alcohols, suggesting that these receptors may be another physiological target for these compounds. The modulation is dependent upon the molecular volume of the compound, further supporting the concept of an anesthetic binding pocket of limited volume common on other Cys-loop ligand-gated ion channels. Incorporation of the 5-HT3B subunit alters either the anesthetic binding site or the allosteric interactions between anesthetic binding and channel opening.
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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.