The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands |
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| Authors: | Bojarski Andrzej J Duszyńska Beata Ko?aczkowski Marcin Kowalski Piotr Kowalska Teresa |
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| Institution: | Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, 12 Smetna Street, 31-343 Kraków, Poland. bojarski@if-pan.krakow.pl |
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| Abstract: | New cis-, trans-2-butene and 1,2-bismethylbenzene analogues of MM77 and NAN-190 (1-4-4-(2-methoxyphenyl)-piperazin-1-yl]-butyl]-pyrrolidine-2,5-dione and isoindole-1,3-dione, respectively) were synthesized. The differences in their in vitro affinity for serotonin 5-HT(7) and 5-HT(1A) receptors were explained using a conformational analysis. A bioactive conformation of those compounds for the 5-HT(7) receptor, different from that established for 5-HT(1A), was proposed. |
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