112947-93-0Relevant articles and documents
Arylalkylamine-, β-carboline-, quinolizine- and azecine-derived compounds and their in vitro interaction with the ionotropic 5-HT3 receptor: Search for new lead structures
Enzensperger, Christoph,Lehmann, Jochen,Von Schroetter, Katrin,Riyazi, Anja,Verspohl, Eugen J.
, p. 544 - 552 (2011/05/11)
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 β-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-HT3 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. ECV · Editio Cantor Verlag.