744252-79-7Relevant academic research and scientific papers
Synthesis and binding properties of novel selective 5-HT3 receptor ligands
Modica, Maria,Romeo, Giuseppe,Materia, Luisa,Russo, Filippo,Cagnotto, Alfredo,Mennini, Tiziana,Gaspar, Robert,Falkay, George,Fueloep, Ferenc
, p. 3891 - 3901 (2004)
This work reports on the synthesis and affinities for the 5-HT3 versus the 5-HT4 receptor of new piperazinyl-substituted thienopyrimidine derivatives 20-45 with a view to identify potent and selective ligands for the 5-HT3 receptor. Some of the new compounds show good affinity for the 5-HT3 receptor and, notably, do not display any affinity for the 5-HT4 receptor. 4-(4-Methyl-1-piperazinyl)-2- methylthio-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidine 31 exhibits the highest affinity for the 5-HT3 receptor (Ki=33nM) and behaves as noncompetitive antagonist.
