ArticleNeuropharmacology2013
Agonists and antagonists induce different palonosetron dissociation rates in 5-HT₃A and 5-HT₃AB receptors.
Article in Neuropharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
12 citing papers in PubMed, 29 citations in OpenAlex.
- Kinetic Benefit(s) of Allosteric Receptor Blockade by Positive Allosteric Modulator Antagonists.ACS pharmacology & translational science · 2026Review
- Focal pharmacological manipulation of serotonin signaling in the amygdala does not alter social behavior.Psychopharmacology · 2025Article
- Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition.Nature reviews. Drug discovery · 2024Review
- 5-HTACS chemical neuroscience · 2022Article
- Development of 3-(4-Chlorophenyl)-1-(phenethyl)urea Analogues as Allosteric Modulators of the Cannabinoid Type-1 Receptor: RTICBM-189 is Brain Penetrant and Attenuates Reinstatement of Cocaine-Seeking Behavior.Journal of medicinal chemistry · 2022Article
- A Single Mutation in the Outer Lipid-Facing Helix of a Pentameric Ligand-Gated Ion Channel Affects Channel Function Through a Radially-Propagating Mechanism.Frontiers in molecular biosciences · 2021Article
- Structure, Function and Physiology of 5-Hydroxytryptamine Receptors Subtype 3.Sub-cellular biochemistry · 2021Review
- High-resolution structures of multiple 5-HTeLife · 2020Article
- Molecular mechanism of setron-mediated inhibition of full-length 5-HTNature communications · 2019Article
- 5-Hydroxytryptamine (5-HT) cellular sequestration during chronic exposure delays 5-HT3 receptor resensitization due to its subsequent release.The Journal of biological chemistry · 2014Article
- Effects of pretreatment with intravenous palonosetron for propofol-remifentanil-based anesthesia in breast and thyroid cancer surgery: a double-blind, randomized, controlled study.Korean journal of anesthesiology · 2014Article
- Exploring a potential palonosetron allosteric binding site in the 5-HT(3) receptor.Bioorganic & medicinal chemistry · 2013Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
Palonosetron is a potent 5-HT₃ receptor antagonist with a unique structure and some unusual properties. Here we explore the properties of palonosetron at heterologously expressed 5-HT₃A and 5-HT₃AB receptors. We used receptors expressed in HEK293 cells, and functionally analysed them using a membrane potential sensitive dye in a Flexstation, which revealed IC₅₀s of 0.24 nM and 0.18 nM for 5-HT₃A and 5-HT₃AB receptors respectively. Radioligand binding studies with [(3)H]palonosetron revealed similar Kds: 0.34 nM for 5-HT3A and 0.15 nM for 5-HT₃AB receptors. Kinetic studies showed palonosetron association and dissociation rates were slightly faster in 5-HT₃AB than 5-HT₃A receptors, and for both subtypes dissociation rates were ligand-dependent, with antagonists causing more rapid dissociation than agonists. Similar ligand effects were not observed for [(3)H]granisetron dissociation studies. These data support previous studies which show palonosetron has actions distinct to other 5-HT3 receptor antagonists, and the slow rates observed for agonist induced dissociation (t₁/₂ > 10 h) could at least partly explain the long duration of palonosetron effects in vivo.
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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.