This work reports on the synthesis and affinities for the 5-HT3 versus the 5-HT4 receptor of new piperazinyl-substitutedthienopyrimidine derivatives 20–45 with a view to identify potent and selective ligands for the 5-HT3 receptor. Some of the newcompounds 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-HT3receptor (Ki ¼ 33 nM) and behaves as noncompetitive antagonist.
Synthesis and binding properties of novel selective 5-HT3 receptor ligands
MODICA, Maria Nunziata;ROMEO, Giuseppe;
2004-01-01
Abstract
This work reports on the synthesis and affinities for the 5-HT3 versus the 5-HT4 receptor of new piperazinyl-substitutedthienopyrimidine derivatives 20–45 with a view to identify potent and selective ligands for the 5-HT3 receptor. Some of the newcompounds 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-HT3receptor (Ki ¼ 33 nM) and behaves as noncompetitive antagonist.File in questo prodotto:
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