Synthesis and binding properties of novel selective 5-HT3 receptor ligands
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...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2004
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| Sorozat: | BIOORGANIC & MEDICINAL CHEMISTRY
12 No. 14 |
| doi: | 10.1016/j.bmc.2004.04.043 |
| mtmt: | 1013248 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/16162 |
| Tartalmi kivonat: | 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 (K-i = 33 nM) and behaves as noncompetitive antagonist. (C) 2004 Elsevier Ltd. All rights reserved. |
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| Terjedelem/Fizikai jellemzők: | 3891-3901 |
| ISSN: | 0968-0896 |