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5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS

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Abstract

5-Aza analogs were prepared of several tryptamine derivatives and a skatole derivative known to bind at human 5-HT6 receptors and evaluated to determine if they bind in a manner similar to their indolic analogs. In general, the azatryptamines did not behave exactly like their tryptamine counterparts, but the behavior of N1-benzenesulfonyl analogs was reminiscent of the known arylsulfonyltryptamines. For example, N1-(4-aminobenzenesulfonyl)-5-azaskatole (18; Ki = 41 nM) displayed an affinity comparable to N1-(4-aminobenzenesulfonyl)skatole.

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Authors and Affiliations

  1. Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA, 23298-0540

    Manik Pullagurla, Małgorzata Dukat & Richard A. Glennon

  2. Department of Psychiatry, School of Medicine, Case Western Reserve University, Cleveland, Ohio, 44106

    Bryan L. Roth & Vincent Setola

  3. Department of Neurosciences, School of Medicine, Case Western Reserve University, Cleveland, Ohio, 44106

    Bryan L. Roth

Authors
  1. Manik Pullagurla
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  2. Małgorzata Dukat
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  3. Bryan L. Roth
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  4. Vincent Setola
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  5. Richard A. Glennon
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Correspondence to Richard A. Glennon.

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Pullagurla, M., Dukat, M., Roth, B. et al. 5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS. Med Chem Res 14, 1–18 (2005). https://doi.org/10.1007/s00044-004-0121-8

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  • DOI: https://doi.org/10.1007/s00044-004-0121-8

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