ArticleMolecular pharmacology2011
Binding sites for bilobalide, diltiazem, ginkgolide, and picrotoxinin at the 5-HT3 receptor.
Article in Molecular pharmacology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 35 citations in OpenAlex.
- Bilobalide increases SKBMC complementary medicine and therapies · 2026Article
- International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.Pharmacological reviews · 2021Review
- Structure, Function and Physiology of 5-Hydroxytryptamine Receptors Subtype 3.Sub-cellular biochemistry · 2021Review
- Bupropion Inhibits Serotonin Type 3AB Heteromeric Channels at Clinically Relevant Concentrations.Molecular pharmacology · 2020Article
- The L-type voltage-gated calcium channel CaLearning & memory (Cold Spring Harbor, N.Y.) · 2017Article
- Noncompetitive Inhibition of 5-HT3 Receptors by Citral, Linalool, and Eucalyptol Revealed by Nonlinear Mixed-Effects Modeling.The Journal of pharmacology and experimental therapeutics · 2016Article
- 5-HT3 Receptor Brain-Type B-Subunits are Differentially Expressed in Heterologous Systems.ACS chemical neuroscience · 2015Article
- Identification of Glycyrrhiza as the rikkunshito constituent with the highest antagonistic potential on heterologously expressed 5-HT3A receptors due to the action of flavonoids.Frontiers in pharmacology · 2015Article
- An atypical residue in the pore of Varroa destructor GABA-activated RDL receptors affects picrotoxin block and thymol modulation.Insect biochemistry and molecular biology · 2014Article
- Phenylalanine in the pore of the Erwinia ligand-gated ion channel modulates picrotoxinin potency but not receptor function.Biochemistry · 2014Article
- Neuroprotective effects of bilobalide on cerebral ischemia and reperfusion injury are associated with inhibition of pro-inflammatory mediator production and down-regulation of JNK1/2 and p38 MAPK activation.Journal of neuroinflammation · 2014Article
- The Concise Guide to PHARMACOLOGY 2013/14: ligand-gated ion channels.British journal of pharmacology · 2013Article
- A golden approach to ion channel inhibition.Trends in pharmacological sciences · 2013Article
- A single channel mutation alters agonist efficacy at 5-HT3A and 5-HT3AB receptors.British journal of pharmacology · 2013Article
- Structure-activity relationships of quinoxaline-based 5-HT3A and 5-HT3AB receptor-selective ligands.ChemMedChem · 2013Article
- Discriminating between 5-HT₃A and 5-HT₃AB receptors.British journal of pharmacology · 2013Review
- Applying linear and non-linear methods for parallel prediction of volume of distribution and fraction of unbound drug.PloS one · 2013Article
- Mixed antagonistic effects of the ginkgolides at recombinant human ρ1 GABAC receptors.Neuropharmacology · 2012Article
- The pharmacological profile of ELIC, a prokaryotic GABA-gated receptor.Neuropharmacology · 2012Article
- Azemiopsin from Azemiops feae viper venom, a novel polypeptide ligand of nicotinic acetylcholine receptor.The Journal of biological chemistry · 2012Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Bilobalide (BB), ginkgolide B (GB), diltiazem (DTZ), and picrotoxinin (PXN) are 5-hydroxytryptamine type 3 (5-HT(3)) receptor antagonists in which the principal sites of action are in the channel. To probe their exact binding locations, 5-HT(3) receptors with substitutions in their pore lining residues were constructed (N-4'Q, E-1'D, S2'A, T6'S, L7'T, L9'V, S12'A, I16'V, D20'E), expressed in Xenopus laevis oocytes, and the effects of the compounds on 5-HT-induced currents were examined. EC(50) values at mutant receptors were less than 6-fold different from those of wild type, indicating that the mutations were well tolerated. BB, GB, DTZ, and PXN had pIC(50) values of 3.33, 3.14, 4.67, and 4.97, respectively. Inhibition by BB and GB was abolished in mutant receptors containing T6'S and S12'A substitutions, but their potencies were enhanced (42- and 125-fold, respectively) in S2'A mutant receptors. S2'A substitution also caused GB ligand trap. PXN potency was modestly enhanced (5-fold) in S2'A, abolished in T6'S, and reduced in L9'V (40-fold) and S12'A (7-fold) receptors. DTZ potency was reduced in L7'T and S12'A receptors (5-fold), and DTZ also displaced [(3)H]granisetron binding, indicating mixed competitive/noncompetitive inhibition. We conclude that regions close to the hydrophobic gate of M2 are important for the inhibitory effects of BB, GB, DTZ, and PXN at the 5-HT(3) receptor; for BB, GB, and PXN, the data show that the 6' channel lining residue is their major site of action, with minor roles for 2', 9', and 12' residues, whereas for DTZ, the 7' and 12' sites are important.
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