868632-01-3Relevant academic research and scientific papers
Synthesis and receptor binding of new thieno[2,3-d]-pyrimidines as selective ligands of 5-HT3 receptors
Modica, Maria N.,Romeo, Giuseppe,Salerno, Loredana,Pittala, Valeria,Siracusa, Maria A.,Mereghetti, Ilario,Cagnotto, Alfredo,Mennini, Tiziana,Gaspar, Robert,Gal, Adrienn,Falkay, George,Palko, Marta,Maksay, Gabor,Fueluep, Ferenc
experimental part, p. 333 - 343 (2009/04/04)
With the aim to develop new potent and selective ligands of 5-HT 3-type serotonin receptors and to acquire more information on their structure-affinity relationships, new thieno[2,3-d]pyrimidine derivatives 32-39 were synthesized and their binding to 5-HT3 versus 5-HT4 receptors was studied. Some of these new compounds exhibit good affinity for cortical 5-HT3 receptors, but not for 5-HT4 receptors. Among these derivatives, 6-ethyl-4-(4-methyl-1-piperazinyl)-2-(methylthio)- thieno[2,3-d]pyrimidine 32 is the most potent ligand (Ki = 67 nM); it behaves as a competitive antagonist of the 5-HT3 receptor function in the guinea pig colon. Its binding interactions with 5-HT3A receptors were analysed by using receptor modelling and comparative docking.
