Synthesis and receptor binding of new thieno[2,3-d]pyrimidines as selective ligands of 5-HT3 receptors
With the aim to develop new potent and selective ligands of 5-HT3-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...
Elmentve itt :
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2008
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| Sorozat: | ARCHIV DER PHARMAZIE
341 No. 6 |
| doi: | 10.1002/ardp.200700205 |
| mtmt: | 1127905 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/16155 |
| LEADER | 01954nab a2200361 i 4500 | ||
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| 005 | 20190719120828.0 | ||
| 008 | 190719s2008 hu o 0|| zxx d | ||
| 022 | |a 0365-6233 | ||
| 024 | 7 | |a 10.1002/ardp.200700205 |2 doi | |
| 024 | 7 | |a 1127905 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a zxx | ||
| 100 | 1 | |a Modica Maria N. | |
| 245 | 1 | 0 | |a Synthesis and receptor binding of new thieno[2,3-d]pyrimidines as selective ligands of 5-HT3 receptors |h [elektronikus dokumentum] / |c Modica Maria N. |
| 260 | |c 2008 | ||
| 300 | |a 333-343 | ||
| 490 | 0 | |a ARCHIV DER PHARMAZIE |v 341 No. 6 | |
| 520 | 3 | |a With the aim to develop new potent and selective ligands of 5-HT3-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-l-piperazinyl)-2-(methylthio)thieno[2,3-d]pyrimidine 32 is the most potent ligand (K-i = 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. | |
| 700 | 0 | 1 | |a Romeo Giuseppe |e aut |
| 700 | 0 | 1 | |a Salerno Loredana |e aut |
| 700 | 0 | 1 | |a Pittala Valeria |e aut |
| 700 | 0 | 1 | |a Siracusa Maria A. |e aut |
| 700 | 0 | 1 | |a Mereghetti Ilario |e aut |
| 700 | 0 | 1 | |a Cagnotto Alfredo |e aut |
| 700 | 0 | 1 | |a Mennini Tiziana |e aut |
| 700 | 0 | 1 | |a Gáspár Róbert |e aut |
| 700 | 0 | 1 | |a Gál Adrienn |e aut |
| 700 | 0 | 1 | |a Falkay György |e aut |
| 700 | 0 | 1 | |a Palkó Márta |e aut |
| 700 | 0 | 1 | |a Maksay Gábor |e aut |
| 700 | 0 | 1 | |a Fülöp Ferenc |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/16155/1/ModicaArchPharmChemLifeSci2008.pdf |z Dokumentum-elérés |