The impact of spacer structure on 5-HT 7 and 5-HT 1A receptor affinity in the group of long-chain arylpiperazine ligands

…, B Duszyńska, M Kołaczkowski, P Kowalski…

Index: Bojarski, Andrzej J.; Duszynska, Beata; Kolaczkowski, Marcin; Kowalski, Piotr; Kowalska, Teresa Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 23 p. 5863 - 5866

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Citation Number: 37

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- HT7 and 5-HT1A receptors were explained using a conformational analysis. A bioactive conformation of those compounds for the 5-HT7 receptor, different from that established ...