Azabicycloalkyl benzimidazolone derivatives as a novel class of potent agonists at the 5-HT sub(4) receptor positively coupled to adenylate cyclase in brain

In this study the ability of three azabicycloalkyl benzimidazolone derivatives, BIMU 1, BIMU 8, and DAU 6215 (structural formulas are given in the text), to stimulate cAMP formation in colliculi neurons in primary culture have been tested. Two of the compounds, BIMU 1 and BIMU 8, which show prokinet...

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Published in:Naunyn-Schmiedeberg's archives of pharmacology 1991-01, Vol.343 (3), p.245-251
Main Authors: Dumuis, A, Sebben, M, Monferini, E, Nicola, M, Turconi, M, Ladinsky, H, Bockaert, J
Format: Article
Language:English
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Summary:In this study the ability of three azabicycloalkyl benzimidazolone derivatives, BIMU 1, BIMU 8, and DAU 6215 (structural formulas are given in the text), to stimulate cAMP formation in colliculi neurons in primary culture have been tested. Two of the compounds, BIMU 1 and BIMU 8, which show prokinetic activity in various animal models, were also good agonists at the 5-HT sub(4) receptors, whereas DAU 6215, a drug devoid of prokinetic activity, was only a weak, partial agonist at 5-HT sub(4) receptors. The activities of the azabicycloalkyl benzimidazolone derivatives and 5-HT on cAMP formation were not additive and ICS 205-930 antagonized the stimulatory effect of these compounds with low potency, further strengthening the notion of interaction with 5-HT sub(4) receptors.
ISSN:0028-1298