ArticleBritish journal of pharmacology2007
The antimalarial drugs quinine, chloroquine and mefloquine are antagonists at 5-HT3 receptors.
Article in British journal of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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Who cites it
26 citing papers in PubMed, 47 citations in OpenAlex.
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- A Case of Post-malarial Postural Orthostatic Tachycardia Syndrome in a Young Woman of South Asian Origin.Cureus · 2024Article
- An In Silico and In Vitro Assessment of the Neurotoxicity of Mefloquine.Biomedicines · 2024Article
- The Nociceptive and Inflammatory Responses Induced by the Ehrlich Solid Tumor Are Changed in Mice Healed ofJournal of parasitology research · 2024Article
- Predicted structure of fully activated human bitter taste receptor TAS2R4 complexed with G protein and agonists.QRB discovery · 2021Article
- Efficacy of THN201, a Combination of Donepezil and Mefloquine, to Reverse Neurocognitive Deficits in Alzheimer's Disease.Frontiers in neuroscience · 2020Article
- Evidence for an effect of receptor density on ligand occupancy and agonist ECScientific reports · 2019Article
- The Effects of Quinine on Neurophysiological Properties of Dopaminergic Neurons.Neurotoxicity research · 2018Article
- Effects of Quinine, Quinidine and Chloroquine on Human Muscle Nicotinic Acetylcholine Receptors.Frontiers in pharmacology · 2018Article
- Article
- Building a 5-HT3A Receptor Expression Map in the Mouse Brain.Scientific reports · 2017Article
- Potentiation of Amitriptyline Anti-Hyperalgesic-Like Action By Astroglial Connexin 43 Inhibition in Neuropathic Rats.Scientific reports · 2016Article
- Prolonged neuropsychiatric effects following management of chloroquine intoxication with psychotropic polypharmacy.Clinical case reports · 2015Article
- Mefloquine and psychotomimetics share neurotransmitter receptor and transporter interactions in vitro.Psychopharmacology · 2014Article
- The antimalarial drug quinine interferes with serotonin biosynthesis and action.Scientific reports · 2014Article
- Discriminating between 5-HT₃A and 5-HT₃AB receptors.British journal of pharmacology · 2013Review
- VUF10166, a novel compound with differing activities at 5-HT₃A and 5-HT₃AB receptors.The Journal of pharmacology and experimental therapeutics · 2012Article
- Cysteine modification reveals which subunits form the ligand binding site in human heteromeric 5-HT3AB receptors.The Journal of physiology · 2011Article
- Mefloquine damage vestibular hair cells in organotypic cultures.Neurotoxicity research · 2011Article
- Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor.Molecular pharmacology · 2011Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeThe antimalarial compounds quinine, chloroquine and mefloquine affect the electrophysiological properties of Cys-loop receptors and have structural similarities to 5-HT(3) receptor antagonists. They may therefore act at 5-HT(3) receptors. EXPERIMENTAL APPROACH: The effects of quinine, chloroquine and mefloquine on electrophysiological and ligand binding properties of 5-HT(3A) receptors expressed in HEK 293 cells and Xenopus oocytes were examined. The compounds were also docked into models of the binding site. KEY
results5-HT(3) responses were blocked with IC (50) values of 13.4 microM, 11.8 microM and 9.36 microM for quinine, chloroquine and mefloquine. Schild plots indicated quinine and chloroquine behaved competitively with pA (2) values of 4.92 (K (B)=12.0 microM) and 4.97 (K (B)=16.4 microM). Mefloquine displayed weakly voltage-dependent, non-competitive inhibition consistent with channel block. On and off rates for quinine and chloroquine indicated a simple bimolecular reaction scheme. Quinine, chloroquine and mefloquine displaced [(3)H]granisetron with K (i) values of 15.0, 24.2 and 35.7 microM. Docking of quinine into a homology model of the 5-HT(3) receptor binding site located the tertiary ammonium between W183 and Y234, and the quinoline ring towards the membrane, stabilised by a hydrogen bond with E129. For chloroquine, the quinoline ring was positioned between W183 and Y234 and the tertiary ammonium stabilised by interactions with F226. CONCLUSIONS AND IMPLICATIONS: This study shows that quinine and chloroquine competitively inhibit 5-HT(3) receptors, while mefloquine inhibits predominantly non-competitively. Both quinine and chloroquine can be docked into a receptor binding site model, consistent with their structural homology to 5-HT(3) receptor antagonists.
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