Arylalkylamine-, beta-carboline-, quinolizine- and azecine-derived compounds and their in vitro interaction with the ionotropic 5-HT3 receptor: search for new lead structures.
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| Abstract |
Specific serotonin receptor agonists and antagonists are marketed with respect to various diseases, most prominently severe emesis. To identify new chemical classes with affinity for the serotonin 5-HT3 channel, several compounds were synthesized which can be structurally classified as arylalkylamines, azecines, quinolizines and beta-carbolines. These were tested in three models: (1) direct effect on ileum (overall model for contracting or relaxant effect), (2) antiserotoninergic effects on rat ileum (crude serotonin model), (3) inhibitory effect on the 5-HT, receptor channel complex expressed in N1E-115 cells (serotonin-induced [14C]guanidinium influx (specific model)). Key findings and conclusion: Several azecine-type compounds exhibit 5-HT3 receptor channel antagonistic properties at concentrations close to that of tropisetron (used as a positive control) and might serve as potential lead structures for the development of further 5-HT3 channel receptor antagonists.
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| Authors | Christoph Enzensperger, Jochen Lehmann, Katrin von Schroetter, Anja Riyazi, Eugen J Verspohl |
| Journal | Arzneimittel-Forschung (Arzneimittelforschung) Vol. 60 Issue 9 Pg. 544-52 ( 2010) ISSN: 0004-4172 [Print] Germany |
| PMID | 21117497 (Publication Type: Journal Article) |
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