ArticleNaunyn-Schmiedeberg's archives of pharmacology2007
Demonstration of 5-HT(3) receptor function and expression in the mouse bladder.
Article in Naunyn-Schmiedeberg's archives of pharmacology, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
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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.
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Who cites it
3 citing papers in PubMed, 17 citations in OpenAlex.
- Ferroptosis in Septic Cardiomyopathy Is Alleviated by Ondansetron: The Critical Role of the HTR3A-ATF3 Axis in Mitochondrial and Oxidative Homeostasis.Biomedicines · 2026Article
- 5-Chloroindole: a potent allosteric modulator of the 5-HT₃ receptor.British journal of pharmacology · 2013Article
- Signal transduction underlying the control of urinary bladder smooth muscle tone by muscarinic receptors and beta-adrenoceptors.Naunyn-Schmiedeberg's archives of pharmacology · 2008Review
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The aim of this study was to demonstrate the presence of 5-HT(3) receptors in the mouse bladder and to determine their location. Bladder strips from female mice were set up in gassed Krebs-Henseleit solution at 37 degrees C and contractions recorded in response to electrical field stimulation (8 Hz, 60 V, 0.5-ms pulse duration) applied for 2 s every 50 s. The potentiating effects of 5-hydroxytryptamine (5-HT) were recorded (in the presence of 1-microM methysergide and 1-microM GR125487 to isolate the 5-HT(3) receptor response), and contractions were expressed as a percentage of the response to 0.1-M KCl. Responses to (5-HT) were also obtained in the presence of the 5-HT(3) receptor antagonist, ondansetron. RT-PCR was used to detect the expression of the 5-HT(3A) and 5-HT(3B) subunit transcripts of the mouse 5-HT(3) receptor. 5-HT and 5-HT(3) receptor agonists caused concentration-dependent increases in the force of neurogenic contractions without affecting the baseline tone. The rank order of potency was: meta-chloro-phenylbiguanide (m-CPB) = 5-HT > 2-methyl-5-HT (2m5-HT) = 1-phenylbiguanide (1-PBG). The respective pEC(50) values were: 6.42 +/- 0.2 = 5.95 +/- 0.19 > 5.35 +/- 0.12 = 5.14 +/- 0.13. m-CPB acted as a full agonist (E (max) = 40.65 +/- 3.81% KCl), but both 2m5-HT and 1-PBG acted as lower potency partial agonists. Ondansetron (30, 100, 300 nM) caused concentration-related rightward displacements to the concentration-effect curve to 5-HT. Nonlinear regression analysis of the effect of the ondansetron concentrations on the pEC(50) values produced a pK(B) value of 8.29 +/- 0.22. Desensitization of sensory nerves to the contractile effect of capsaicin (10 microM for 60 min) did not alter the ability of 5-HT to potentiate neurogenic contractions. 5-HT (3 microM) inhibited contractions induced by direct muscle stimulation (lignocaine, 300 microM and 10-ms pulse width). m-CPB also caused the same effect with a pIC(50) of 6.62 +/- 0.10 and an E (max) of 48.03 +/- 2.25%. The concentration-response curve to m-CPB was shifted rightwards by ondansetron (1 microM) giving an apparent pK(B) value of 8.15 +/- 0.33. mRNA for both the 5-HT(3A) and 5-HT(3B) receptor subunits was detected in the detrusor as well as the mucosa with a greater relative expression of the 5-HT(3A) subunit in both layers. This study demonstrates that 5-HT mediates enhanced neurogenic contractions of the mouse bladder muscle by an action at 5-HT(3) receptors located prejunctionally on nonsensory nerve elements. Additionally, an inhibitory postjunctional population of the 5-HT(3) receptor was identified. The presence of the 5-HT(3) receptor was confirmed by the expression of both 5-HT(3A) and 5-HT(3B) receptor subunits of the 5-HT(3) receptor.
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Registered trials
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