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Acta Physiologica Congress

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Acta Physiologica 2013; Volume 207, Supplement 694
92nd Annual Meeting of the German Physiological Society
3/2/2013-3/5/2013
Heidelberg, Germany


APOMORPHINE IS A BIMODAL MODULATOR OF TRANSIENT RECEPTOR POTENTIAL A 1 (TRPA1) CHANNELS
Abstract number: P115

Schulze 1   *A. , Schaefer 1  M., Hill 1  K.

1 Universität Leipzig, Medizinische Fakultät, Rudolf-Boehm-Institut für Pharmakologie und Toxikologie, Leipzig, Germany

Apomorphine, a dopamine receptor agonist, is clinically used to treat “off-states” in patients suffering from Parkinson's disease. Side effects that arise during therapy include gastrointestinal complications, such as severe emesis and nausea, but also local effects such as ulceration and pain at the injection site.

Here, we provide evidence that the irritant receptor TRPA1 (transient receptor potential ankyrin 1), which is activated by a variety of proalgesic agents, environmental irritants and pungent dietary compounds, may confer some of the adverse responses to apomorphine treatment. Other sensory TRP channels (TRPV1, TRPV2, TRPV4, TRPM3, and TRPM8) were not affected by apomorphine application. The modulation of heterologously expressed TRPA1 by apomorphine was concentration-dependent with an irreversible activation in the low micromolar range and a voltage-dependent inhibition of TRPA1 channels at higher drug concentrations. Furthermore, apomorphine also acted on endogenous TRPA1 in rat dorsal root ganglion neurones and in the human enterochromaffin model cell line QGP-1. Challenging QGP-1 cells with apomorphine caused TRPA1-dependent increases in intracellular calcium and serotonin release.

Taken together, we demonstrate that, besides its known effect on dopamine receptors, apomorphine also activates TRPA1 channels, suggesting that adverse side effects such as nausea and local pain may rely on TRPA1 activation in enterochromaffin cells and sensory neurones, respectively.

To cite this abstract, please use the following information:
Acta Physiologica 2013; Volume 207, Supplement 694 :P115

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