| Autor: |
A, Orjales, L, Alonso-Cires, P L, López-Tudanca, I, Tapia, L, Labeaga, R, Mosquera |
| Rok vydání: |
2000 |
| Předmět: |
|
| Zdroj: |
Drug design and discovery. 16(4) |
| ISSN: |
1055-9612 |
| Popis: |
A series of quinolinecarboxylic acid amides and an ester with a quinuclidine moiety were synthesized and their in vitro affinities at 5-HT3, 5-HT4, and D2 receptors evaluated by radioligand binding assays. Highest affinity at 5-HT3 receptor corresponded to derivative 5 with Ki = 9.9 nM and with selectivity over 5-HT4 and D2 receptors. Compounds displayed moderate 5-HT3 antagonist activity (ED50 = 10.5-21.5 microg/kg i.v.). The obtained data suggest that the 5-HT3 receptor sites can accommodate the acyl group of the 2-quinoline derivatives. The results indicate the existence of an optimal distance between the lone electron pair of the quinoline nitrogen atom and the azabicyclic nitrogen atom, and a no-pharmacophoric pocket in the 5-HT3 receptor which would hold the fragment at the position 4 of the quinoline ring. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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