Evidence map›Paper›PMID 27108935›Full record

ArticleNeuropharmacology2016

The muscarinic antagonists scopolamine and atropine are competitive antagonists at 5-HT3 receptors.

Martin Lochner, Andrew J Thompson

Open access · hybridAbstract read
In one paragraph

Article in Neuropharmacology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 40 papers.

0numbers the graph read from it
0cells of the map it votes in
40citing papers in PubMed
8.5field-weighted citation impact, top 3% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

40 citing papers in PubMed, 73 citations in OpenAlex.

  1. Article
  2. Review
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  4. Therapeutic potential ofFrontiers in behavioral neuroscience · 2026
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  5. Pharmaceuticals (Basel, Switzerland) · 2025
    Article
  6. Review
  7. Review
  8. Review
  9. Article
  10. Article
  11. Administration of Nicotine Can Inhibit Myopic Growth in Animal Models.Investigative ophthalmology & visual science · 2024
    Article
  12. Phytoconstituents Targeting the Serotonin 5-HTACS pharmacology & translational science · 2024
    Review
  13. Article
  14. Article
  15. Article
  16. Article
  17. Article
  18. Article
  19. Review
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

2 authors at 2 institutions in 2 countries.

Martin LochnerDepartment of Chemistry and Biochemistry, University of Bern, Freiestrasse 3, Bern, CH-3012, Switzerland. Electronic address: martin.lochner@dcb.unibe.ch.
Andrew J ThompsonDepartment of Pharmacology, Tennis Court Road, Cambridge, CB2 1PD, UK. Electronic address: ajt44@cam.ac.uk.
Lawn Tennis Association · GBUniversity of Bern · CH

Funding

British Heart Foundation PG/13/39/30293
6 · The paper itself

Abstract

Scopolamine is a high affinity muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. 5-HT3 receptor antagonists are used for the same purpose and are structurally related to scopolamine. To examine whether 5-HT3 receptors are affected by scopolamine we examined the effects of this drug on the electrophysiological and ligand binding properties of 5-HT3A receptors expressed in Xenopus oocytes and HEK293 cells, respectively. 5-HT3 receptor-responses were reversibly inhibited by scopolamine with an IC50 of 2.09 μM. Competitive antagonism was shown by Schild plot (pA2 = 5.02) and by competition with the 5-HT3 receptor antagonists [(3)H]granisetron (Ki = 6.76 μM) and G-FL (Ki = 4.90 μM). The related molecule, atropine, similarly inhibited 5-HT evoked responses in oocytes with an IC50 of 1.74 μM, and competed with G-FL with a Ki of 7.94 μM. The reverse experiment revealed that granisetron also competitively bound to muscarinic receptors (Ki = 6.5 μM). In behavioural studies scopolamine is used to block muscarinic receptors and induce a cognitive deficit, and centrally administered concentrations can exceed the IC50 values found here. It is therefore possible that 5-HT3 receptors are also inhibited. Studies that utilise higher concentrations of scopolamine should be mindful of these potential off-target effects.

Indexed as

AnimalsAtropineBinding, CompetitiveDose-Response Relationship, DrugFemaleGuinea PigsHEK293 CellsHumansMaleMuscarinic AntagonistsProtein Structure, SecondaryProtein Structure, TertiaryReceptors, Serotonin, 5-HT3ScopolamineSerotonin 5-HT3 Receptor AntagonistsXenopus laevisAtropineMuscarinic AntagonistsReceptors, Serotonin, 5-HT3ScopolamineSerotonin 5-HT3 Receptor Antagonists5-HT(3)AmygdalaAntagonistAnxietyBinding siteCognitionCys-loopDepressionHippocampusLigand dockingMemoryMuscarinicScopolamine

Identifiers

PMID27108935
PMCPMC4920643
OpenAlexW2335911696

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.