The antimalarial drugs quinine, chloroquine and mefloquine are antagonists at 5-HT 3 receptors

British Journal of Pharmacology

Volumn 151, Issue 5, 2007, Pages 666-677

  Thompson, A J ^a   Lochner, M ^a   Lummis, S C R ^a,b  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

^b Department of Biochemistry ^*  (United Kingdom)

Author keywords

5 HT 3 receptor; Antagonist; Binding site; Chloroquine; Cys loop receptor; Ligand docking; Malaria; Mefloquine; Quinine

Indexed keywords

AMMONIA; ANTIMALARIAL AGENT; CHLOROQUINE; GRANISETRON; LIGAND; MEFLOQUINE; QUININE; SEROTONIN; SEROTONIN 3 ANTAGONIST; SEROTONIN 3 RECEPTOR; SEROTONIN 3A RECEPTOR; SEROTONIN RECEPTOR; TRITIUM; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CELL STRAIN HEK293; COMPETITIVE INHIBITION; CONTROLLED STUDY; DRUG EFFECT; DRUG RECEPTOR BINDING; EMBRYO; FEMALE; HUMAN; HUMAN CELL; HYDROGEN BOND; IC 50; MOLECULAR MODEL; NONHUMAN; NUCLEOTIDE SEQUENCE; OOCYTE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RECEPTOR BLOCKING; SEQUENCE HOMOLOGY; STRUCTURAL HOMOLOGY; XENOPUS;

ALGORITHMS; ANIMALS; ANTIMALARIALS; BINDING, COMPETITIVE; CELLS, CULTURED; CHLOROQUINE; DOSE-RESPONSE RELATIONSHIP, DRUG; ELECTROPHYSIOLOGY; FEMALE; GRANISETRON; KINETICS; MEFLOQUINE; MODELS, MOLECULAR; OOCYTES; QUININE; RADIOLIGAND ASSAY; RECEPTORS, SEROTONIN, 5-HT3; SEROTONIN ANTAGONISTS; XENOPUS LAEVIS;

EID: 34347358557     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1038/sj.bjp.0707238     Document Type: Article

References (41)

1. Arunlakshana O, Schild HO (1959). Some quantitative uses of drug antagonists. Br J Pharmacol Chemother 14: 48-58.
2. Ballestero JA, Plazas PV, Kracun S, Gomez-Casati ME, Taranda J, Rothlin CV et al. (2005). Effects of quinine, quinidine and chloroquine on α9 α10 nicotinic cholinergic receptors. Mol Pharmacol 68: 822-829.
3. 3 receptor cation channels by ifenprodil in excised patches of N1E-115 cells. Naunyn Schmiedebergs Arch Pharmacol 358: 145-152.
4. 3 receptor revealed by unnatural amino acid mutagenesis. J Neurosci 24: 9097-9104.
5. Bray PG, Martin RE, Tilley L, Ward SA, Kirk K, Fidock DA (2005). Defining the role of PfCRT in Plasmodium falciparum chloroquine resistance. Mol Microbiol 56: 323-333.
6. Das P, Bell-Horner CL, Huang RQ, Raut A, Gonzales EB, Chen ZL et al. (2004). Inhibition of type A GABA receptors by L-type calcium channel blockers. Neuroscience 124: 195-206.
7. 3B subunit is a major determinant of serotonin-receptor function. Nature 397: 359-363.
8. 3 receptor-mediated ion current in Xenopus oocytes. Brain Res 673: 181-184.
9. Goldin LR (1992). Maintenance of Xenopus laevis and Oocyte Injection. In: Bernardo R, Iverson LE (eds.) Methods in Enzymology. Academic Press: New York, vol. 207 pp 267-279.
10. 3 receptors. J Physiol 519: 713-722.
11. 2+ channels. Mol Pharmacol 50: 1284-1294.
12. Jordan M, Schallhorn A, Wurm FM (1996). Transfecting mammalian cells: optimization of critical parameters affecting calcium-phosphate precipitate formation. Nucleic Acids Res 24: 596-601.
13. Kearney PC, Nowak MW, Zhong W, Silverman SK, Lester HA, Dougherty DA (1996). Dose-response relations for unnatural amino acids at the agonist binding site of the nicotinic acetylcholine receptor: tests with novel side chains and with several agonists. Mol Pharmacol 50: 1401-1412.
14. 3 receptor-mediated ion current in N1E-115 neuroblastoma cells. Br J Pharmacol 108: 287-289.
15. Leff P, Dougall IG (1993). Further concerns over Cheng-Prusoff analysis. Trends Pharmacol Sci 14: 110-112.
16. Lew MJ, Angus JA (1995). Analysis of competitive agonist-antagonist interactions by nonlinear regression. Trends Pharmacol Sci 16: 328-337.
17. + channel determined by construction of multimeric cDNAs. Neuron 9: 861-871.
18. Lobel HO, Miani M, Eng T, Bernard KW, Hightower AW, Campbell CC (1993). Long-term malaria prophylaxis with weekly mefloquine. Lancet 341: 848-851.
19. 3 receptors in N1E-115 neuroblastoma cells. Eur J Pharmacol 243: 7-11.
20. Luzzi GA, Peto TE (1993). Adverse effects of antimalarials. An update Drug Saf 8: 295-311.
21. 3 receptor. Neuropharmacology 34: 621-629.
22. Neubig RR, Spedding M, Kenakin T, Christopoulos A (2003). International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on terms and symbols in quantitative pharmacology. Pharmacol Rev 55: 597-606.
23. 3 serotonin receptor-like genes HTR3C, HTR3D and HTR3E. Gene 310: 101-111.
24. Olsen L, Pettersson I, Hemmingsen L, Adolph HW, Jorgensen FS (2004). Docking and scoring of metallo-beta-lactamases inhibitors. J Comput Aided Mol Des 18: 287-302.
25. Palmer KJ, Holliday SM, Brogden RN (1993). Mefloquine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic efficacy. Drugs 45: 430-475.
26. Papke RL, Thinschmidt JS (1998). The correction of alpha7 nicotinic acetylcholine receptor concentration-response relationships in Xenopus oocytes. Neurosci Lett 256: 163-166.
27. 3 receptor. J Biol Chem 279: 23294-23301.
28. Ramharter M, Wernsdorfer WH, Kremsner PG (2004). In vitro activity of quinolines against Plasmodium falciparum in Gabon. Acta Trop 90: 55-60.
29. Rammes G, Eisensamer B, Ferrari U, Shapa M, Gimpl G, Gilling K et al. (2004). Antipsychotic drugs antagonize human serotonin type 3 receptor currents in a noncompetitive manner. Mol Psychiatry 9: 846-858.
30. 3 receptor: a model ligand-gated ion channel (review). Mol Membr Biol 19: 11-26.
31. 3 receptor agonist-binding residues using homology modeling. Biophys J 84: 2338-2344.
32. Sali A, Blundell TL (1993). Comparative protein modelling by satisfaction of spatial restraints. J Mol Biol 234: 779-815.
33. Shi J, Blundell TL, Mizuguchi K (2001). FUGUE: sequence-structure homology recognition using environment-specific substitution tables and structure-dependent gap penalties. J Mol Biol 310: 243-257.
34. Sieb JP, Milone M, Engel AG (1996). Effects of the quinoline derivatives quinine, quinidine, and chloroquine on neuromuscular transmission. Brain Res 712: 179-189.
35. 3 receptor. Mol Memb Biol 23: 1-10.
36. Taylor WR, White NJ (2004). Antimalarial drug toxicity: a review. Drug Saf 27: 25-61.
37. 3 receptor F-loop. J Biol Chem 281: 16576-16582.
38. 3 Receptor. In: Roth B (ed.) The serotonin receptors: from molecular pharmacology to human therapeutics pp 439-457.
39. 3 receptor binding site using modeling and radioligand binding. J Biol Chem 280: 20476-20482.
40. Tikhonov DB, Mellor IR, Usherwood PN (2004). Modeling noncompetitive antagonism of a nicotinic acetylcholine receptor. Biophys J 87: 159-170.
41. Uhlemann A, Yuthavong Y, Fidock DA (2005). Mechanisms of Antimalarial Drug Action and Resistance. Sherman IW (ed.) Molecular Approaches to Malaria. ASM Press: Washington, USA, pp 429-461.