Literature DB >> 15501057

The impact of spacer structure on 5-HT7 and 5-HT1A receptor affinity in the group of long-chain arylpiperazine ligands.

Andrzej J Bojarski1, Beata Duszyńska, Marcin Kołaczkowski, Piotr Kowalski, Teresa Kowalska.   

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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Year:  2004        PMID: 15501057     DOI: 10.1016/j.bmcl.2004.09.029

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders.

Authors:  Marcello Leopoldo; Enza Lacivita; Francesco Berardi; Roberto Perrone; Peter B Hedlund
Journal:  Pharmacol Ther       Date:  2010-10-20       Impact factor: 12.310

2.  Synthesis of conformationally constrained aryl- or heteroarylpiperazinyl derivatives of selected imides as 5-HT1A receptor ligands.

Authors:  Jerzy Kossakowski; Mariola Krawiecka; Bozena Kuran
Journal:  Molecules       Date:  2006-08-23       Impact factor: 4.411

  2 in total

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