Please use this identifier to cite or link to this item:
http://dx.doi.org/10.25673/118288
Title: | Cantharidin and sodium fluoride attenuate the negative inotropic effect of the A₁-adenosine receptor agonist N⁶-(R)-phenylisopropyl adenosine in isolated human atria |
Author(s): | Schwarz, Rebecca Lia![]() Hofmann, Britt ![]() Gergs, Ulrich ![]() Neumann, Joachim ![]() |
Issue Date: | 2025 |
Type: | Article |
Language: | English |
Abstract: | Cantharidin and sodium fluoride inhibit the activity of serine/threonine protein phosphatases 1 (PP1) and 2A (PP2A) and increase the force of contraction in human atrial preparations. R-phenylisopropyl adenosine (R-PIA) acts as an agonist at A₁-adenosine receptors. R-PIA exerts a negative inotropic effect on human atria. The effect of R-PIA - and its various manifestations - are currently explained as a function of the inhibition of sarcolemmal adenylyl cyclase activity and/or opening of sarcolemmal potassium channels. We hypothesise that cantharidin and sodium fluoride may attenuate the negative inotropic effect of R-PIA. During open heart surgery, trabeculae carneae from the right atrium were obtained for human atrial preparations (HAPs). These trabeculae were mounted in organ baths and electrically stimulated at 1 Hz. Furthermore, we studied isolated electrically stimulated left atrial (LA) preparations from female wild-type mice (CD1). The force of contraction was recorded under isometric conditions. R-PIA (1 µM) exerted a rapid negative inotropic effect in the HAPs and mice LA preparations. These negative inotropic effects of R-PIA were attenuated by pre-incubation for 30 min with 100-µM cantharidin in HAPs, but not in mice LA preparations. Adenosine signals via A₁ receptors in a species-specific pathway in mammalian atria. We postulate that R-PIA, at least in part, exerts a negative inotropic effect via activation of serine/threonine phosphatases in the human atrium. |
URI: | https://opendata.uni-halle.de//handle/1981185920/120247 http://dx.doi.org/10.25673/118288 |
Open Access: | ![]() |
License: | ![]() |
Journal Title: | Naunyn-Schmiedeberg's archives of pharmacology |
Publisher: | Springer |
Publisher Place: | Berlin |
Volume: | 398 |
Issue: | 2 |
Original Publication: | 10.1007/s00210-024-03402-2 |
Page Start: | 1961 |
Page End: | 1971 |
Appears in Collections: | Open Access Publikationen der MLU |
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File | Description | Size | Format | |
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s00210-024-03402-2.pdf | 1.28 MB | Adobe PDF | ![]() View/Open |