Nyitólap » Imidazoline receptors are not involved in the regulation of gastric motility Imidazoline receptors are not involved in the regulation of gastric motility In the last two decades three different imidazoline receptors I1-I3 have been described, and a considerable weight of evidence has accumulated to suggest that they may be promising therapeutic options for a number of conditions, like hypertension, heart failure, metabolic syndrome, chronic pain, diabetes, depression or neurodegenerative disorders.
Imidazoline receptors have also been identified throughout the gastrointestinal GI tract, so we hypothesized that these receptors may play a role in the regulation of GI motor activity.
Our aim was to find novel targets for the pharmacotherapy of GI disorders accompanied by motility disturbances e. It is rather difficult, however, to distuingish the imidazoline receptor-mediated effects from the α2-adrenoceptor-mediated ones due to the reasonable affinity of most imidazoline ligands for the α2-adrenoceptors.
Therefore, we tested the effect of various imidazoline and α2-adrenoceptor ligands on the electric field stimulated EFS gastric contractions in wild type WTα2A- α2B— and α2C-adrenoceptor knock out KO mice. We found that mixed α2-adrenoceptor and imidazoline receptor agonists like clonidine or rilmenidine produced a concentration-dependent inhibition on the EFS-induced gastric contractions in both WT, α2B— and α2C-adrenoceptor KO mice, but not in α2A-adrenoceptor KO mice.
Thus, we concluded, that gastroparesis pain location both imidazoline receptors and their endogenous ligands agmatine have been identified in the GI tract, they are not involved in the regulation of gastric motor activity.
Each column represents mean ± S. Eur J Pharmacol.