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In Vitro and Direct In Vivo Testing of Mixture-Based Combinatorial Libraries for the Identification of Highly Active and Specific Opiate Ligands

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Drug Addiction

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Abstract

The use of combinatorial libraries for the identification of novel opiate and related ligands in opioid receptor assays is reviewed. Case studies involving opioid assays used to demonstrate the viability of combinatorial libraries are described. The identification of new opioid peptides composed of L-amino acids, D-amino acids, or L-, D-, and unnatural amino acids is reviewed. New opioid compounds have also been identified from peptidomimetic libraries, such as peptoids and alkylated dipeptides, and those identified from acyclic (eg, polyamine, urea) and heterocyclic (eg, bicyclic guanidine) libraries are reviewed.

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Authors and Affiliations

  1. Torrey Pines Institute for Molecular Studies, 3550 General Atomics Court, San Diego, CA, 92121

    Richard A. Houghten, Colette T. Dooley & Jon R. Appel

Authors
  1. Richard A. Houghten
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  2. Colette T. Dooley
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  3. Jon R. Appel
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Correspondence to Richard A. Houghten .

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Editors and Affiliations

  1. National Institute on Drug Abuse, Bethesda, MD, USA

    Rao S. Rapaka

  2. College of Medicine and Public Health, Ohio State University, Columbus, OH, USA

    Wolfgang Sadée

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© 2008 American Association of Pharmaceutical Scientists

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Houghten, R.A., Dooley, C.T., Appel, J.R. (2008). In Vitro and Direct In Vivo Testing of Mixture-Based Combinatorial Libraries for the Identification of Highly Active and Specific Opiate Ligands. In: Rapaka, R.S., Sadée, W. (eds) Drug Addiction. Springer, New York, NY. https://doi.org/10.1007/978-0-387-76678-2_26

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