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  • Title: The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.
    Author: Bojarski AJ, Duszyńska B, Kołaczkowski M, Kowalski P, Kowalska T.
    Journal: Bioorg Med Chem Lett; 2004 Dec 06; 14(23):5863-6. PubMed ID: 15501057.
    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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