ArticleBritish journal of pharmacology2008
Antimalarial drugs inhibit human 5-HT(3) and GABA(A) but not GABA(C) receptors.
Article in British journal of pharmacology, 2008. 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, 52 citations in OpenAlex.
- Commonly Used Therapeutics Associated with Changes in Arousal Inhibit GABABiomolecules · 2023Article
- The next generation of malaria treatments: the great expectations.Future science OA · 2023Article
- Inhibition of connexin hemichannels alleviates neuroinflammation and hyperexcitability in temporal lobe epilepsy.Proceedings of the National Academy of Sciences of the United States of America · 2022Article
- Structure, Function and Physiology of 5-Hydroxytryptamine Receptors Subtype 3.Sub-cellular biochemistry · 2021Review
- Review
- Connexins-Based Hemichannels/Channels and Their Relationship with Inflammation, Seizures and Epilepsy.International journal of molecular sciences · 2019Review
- Natural Negative Allosteric Modulators of 5-HT₃ Receptors.Molecules (Basel, Switzerland) · 2018Review
- Heterologous Expression of a Novel Drug Transporter from the Malaria Parasite Alters Resistance to Quinoline Antimalarials.Scientific reports · 2018Article
- Effects of Quinine, Quinidine and Chloroquine on Human Muscle Nicotinic Acetylcholine Receptors.Frontiers in pharmacology · 2018Article
- Intraglomerular gap junctions enhance interglomerular synchrony in a sparsely connected olfactory bulb network.The Journal of physiology · 2017Article
- The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT3 receptors.Neuropharmacology · 2016Article
- Prolonged neuropsychiatric effects following management of chloroquine intoxication with psychotropic polypharmacy.Clinical case reports · 2015Article
- Gap junctions in the ventral hippocampal-medial prefrontal pathway are involved in anxiety regulation.The Journal of neuroscience : the official journal of the Society for Neuroscience · 2014Article
- 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
- The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.British journal of pharmacology · 2013Article
- 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
- Computational modeling reveals dendritic origins of GABA(A)-mediated excitation in CA1 pyramidal neurons.PloS one · 2012Article
- Cys-loop receptor channel blockers also block GLIC.Biophysical journal · 2011Article
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeAntimalarial compounds have been previously shown to inhibit rodent nicotinic acetylcholine (nACh) and 5-HT(3) receptors. Here, we extend these studies to include human 5-HT(3A), 5-HT(3AB), GABA(A) alpha1beta2, GABA(A) alpha1beta2gamma2 and GABA(C) rho1 receptors. EXPERIMENTAL APPROACH: We examined the effects of quinine, chloroquine and mefloquine on the electrophysiological properties of receptors expressed in Xenopus oocytes. KEY
results5-HT(3A) receptor responses were inhibited by mefloquine, quinine and chloroquine with IC(50) values of 0.66, 1.06 and 24.3 microM. At 5-HT(3AB) receptors, the potencies of mefloquine (IC(50)=2.7 microM) and quinine (15.8 microM), but not chloroquine (23.6 microM), were reduced. Mefloquine, quinine and chloroquine had higher IC(50) values at GABA(A) alpha1beta2 (98.7, 0.40 and 0.46 mM, respectively) and GABA(A) alpha1beta2gamma2 receptors (0.38, 1.69 and 0.67 mM, respectively). No effect was observed at GABA(C) rho1 receptors. At all 5-HT(3) and GABA(A) receptors, chloroquine displayed competitive behaviour and mefloquine was non-competitive. Quinine was competitive at 5-HT(3A) and GABA(A) receptors, but non-competitive at 5-HT(3AB) receptors. Homology modelling in combination with automated docking suggested orientations of quinine and chloroquine at the GABA(A) receptor binding site. CONCLUSIONS AND IMPLICATIONS: The effects of mefloquine, quinine and chloroquine are distinct at GABA(A) and GABA(C) receptors, whereas their effects on 5-HT(3AB) receptors are broadly similar to those at 5-HT(3A) receptors. IC(50) values for chloroquine and mefloquine at 5-HT(3) receptors are close to therapeutic blood concentrations required for malarial treatment, suggesting that their therapeutic use could be extended to include the treatment of 5-HT(3) receptor-related disorders.
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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.