Literature DB >> 9871525

Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors.

B E Maryanoff1, D F McComsey, G E Martin, R P Shank.   

Abstract

We synthesized 20 and 21 as conformationally constrained analogues of the dopamine receptor antagonist SKF-83742, as well as analogues 6-9, 16, and 18-22. Although 20 and 21 were inactive, 7, 9, and 19 showed strong binding to D-1, D-2, S-2, and alpha-1 receptors, as well as antipsychotic activity in vivo.

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Year:  1998        PMID: 9871525     DOI: 10.1016/s0960-894x(98)00138-3

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


  1 in total

1.  Exploring structure-selectivity relationships of biogenic amine GPCR antagonists using similarity searching and dynamic compound mapping.

Authors:  Ingo Vogt; Hany E A Ahmed; Jens Auer; Jürgen Bajorath
Journal:  Mol Divers       Date:  2008-03-04       Impact factor: 2.943

  1 in total

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