The Antimalarial Drug Proguanil Is an Antagonist at 5-HT3 Receptors

No abstract is available for this paper.

• Publication year

  2014

• Venue

  Journal of Pharmacology and Experimental Therapeutics

• Publication date

  2014-12-01

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1124/jpet.114.218461PMID 25277140
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Inhibition of native 5-HT3 receptor-evoked contractions in guinea pig and mouse ileum by antimalarial drugs.

  2014cited by this paper
• Metformin—mode of action and clinical implications for diabetes and cancer

  2014cited by this paper
• X-ray structure of the mouse serotonin 5-HT3 receptor

  2014influential reference
• Which agonist properties are important for the activation of 5-HT3A receptors?

  2013cited by this paper
• Importance of recognition loops B and D in the activation of human 5-HT₃ receptors by 5-HT and meta-chlorophenylbiguanide.

  2013influential reference
• Structural insights into Cys-loop receptor function and ligand recognition.

  2013cited by this paper
• A single channel mutation alters agonist efficacy at 5-HT3A and 5-HT3AB receptors

  2013influential reference
• Partial agonism of 5-HT3 receptors: a novel approach to the symptomatic treatment of IBS-D.

  2013cited by this paper
• New chemotherapeutic strategies against malaria, leishmaniasis and trypanosomiases.

  2013cited by this paper
• Recent developments in 5-HT3 receptor pharmacology.

  2013cited by this paper
• Structural basis of ligand recognition in 5-HT3 receptors

  2012influential reference
• Varenicline Is a Potent Agonist of the Human 5-Hydroxytryptamine3 Receptor

  2011cited by this paper
• The structural basis of function in Cys-loop receptors

  2010cited by this paper
• Novel structural determinants of single channel conductance and ion selectivity in 5‐hydroxytryptamine type 3 and nicotinic acetylcholine receptors

  2010cited by this paper
• Antimalarial drugs inhibit human 5‐HT3 and GABAA but not GABAC receptors

  2008cited by this paper
• A Hydrogen Bond in Loop A Is Critical for the Binding and Function of the 5-HT3 Receptor

  2008cited by this paper
• The antimalarial drugs quinine, chloroquine and mefloquine are antagonists at 5‐HT3 receptors

  2007influential reference
• MD-354: what is it good for?

  2007influential reference
• Estimating Binding Affinities of the Nicotinic Receptor for Low-efficacy Ligands Using Mixtures of Agonists and Two-dimensional Concentration–Response Relationships

  2006cited by this paper
• Molecular cloning and pharmacological characterization of serotonin 5-HT(3A) receptor subtype in dog.

  2006cited by this paper
• In vitro metabolism of phenoxypropoxybiguanide analogues in human liver microsomes to potent antimalarial dihydrotriazines.

  2005cited by this paper
• Effects of Quinine, Quinidine, and Chloroquine on α9α10 Nicotinic Cholinergic Receptors

  2005influential reference
• The loop C region of the murine 5-HT3A receptor contributes to the differential actions of 5-hydroxytryptamine and m-chlorophenylbiguanide.

  2005cited by this paper
• Effects of quinine, quinidine, and chloroquine on alpha9alpha10 nicotinic cholinergic receptors.

  2005cited by this paper
• Docking and scoring of metallo-beta-lactamases inhibitors.

  2004cited by this paper
• Docking and scoring of metallo-β-lactamases inhibitors

  2004cited by this paper
• Single dose pharmacokinetics of proguanil and its metabolites in pregnancy

  2004influential reference
• International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology

  2003cited by this paper
• Co-expression of the 5-HT3B serotonin receptor subunit alters the biophysics of the 5-HT3 receptor.

  2003cited by this paper
• Arylguanidine and arylbiguanide binding at 5-HT3 serotonin receptors: a QSAR study.

  2003cited by this paper
• International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification. XXXVIII. Update on Terms and Symbols in Quantitative Pharmacology

  2003cited by this paper
• Identification of critical residues in loop E in the 5-HT3ASR binding site

  2002cited by this paper
• FUGUE: sequence-structure homology recognition using environment-specific substitution tables and structure-dependent gap penalties.

  2001cited by this paper
• The Role of Tryptophan Residues in the 5-Hydroxytryptamine3 Receptor Ligand Binding Domain*

  2000cited by this paper
• Identification of a domain affecting agonist potency of meta-chlorophenylbiguanide in 5-HT3 receptors.

  1999influential reference
• Binding, gating, affinity and efficacy: The interpretation of structure‐activity relationships for agonists and of the effects of mutating receptors

  1998cited by this paper
• The correction of alpha7 nicotinic acetylcholine receptor concentration-response relationships in Xenopus oocytes.

  1998cited by this paper
• Effects of the quinoline derivatives quinine, quinidine, and chloroquine on neuromuscular transmission.

  1996cited by this paper
• Structure-activity relationships for the binding of arylpiperazines and arylbiguanides at 5-HT3 serotonin receptors.

  1996cited by this paper
• Characterization of a human 5‐hydroxytryptamine3 receptor type A (h5‐HT3R‐AS) subunit stably expressed in HEK 293 cells

  1996cited by this paper
• Analysis of competitive agonist-antagonist interactions by nonlinear regression.

  1995cited by this paper
• International Union of Pharmacology Committee on Receptor Nomenclature and Drug Classification.

  1994cited by this paper
• Accumulation of metformin by tissues of the normal and diabetic mouse.

  1994influential reference
• Prophylaxis against malaria for travellers from the United Kingdom. Malaria Reference Laboratory and the Ross Institute.

  1993cited by this paper
• Further concerns over Cheng-Prusoff analysis.

  1993cited by this paper
• Prophylaxis against malaria for travellers from the United Kingdom. Report of meetings convened by the Malaria Reference Laboratory and the Ross Institute.

  1989cited by this paper
• Single dose pharmacokinetics of proguanil and its metabolites in healthy subjects.

  1987influential reference
• Effects of quinine, proguanil and chloroquine on cardio-vascular responses of adrenaline and acetylcholine in dogs.

  1956cited by this paper
• Effects of quinine, proguanil and chloroquine on cardio-vascular responses of adrenaline and acetylcholine in dogs.

  1956cited by this paper
• Article Title: Loop B Is a Major Structural Component of the 5-HT3

  year unknowncited by this paper

• [Medical treatment of male lower urinary tract symptoms: what's new?]

  2022cites this paper
• Antimalaria Medicine and Its Mechanism : A Review

  2020cites this paper
• A challenge finding P2X1 and P2X4 ligands.

  2019cites this paper
• Evidence for an effect of receptor density on ligand occupancy and agonist EC50

  2019cites this paper