Medicinal Chemistry: New Chemical Classes and Subtype-Selective Ligands

  • Amy Hauck Newman
  • Andrew Coop
Chapter

6. Summary

Over the past decade, advances have been made in discovering novel σ receptor probes and developing structure-activity relationships for σ1 and σ2 receptor selectivity. These compounds have provided useful tools to further investigate the physiological role that central and peripheral σ receptors play. Furthermore, many of these compounds have been investigated for their in vivo actions, and particularly promising is their ability to attenuate cocaine-induced behaviors such as locomotor stimulation and conditioned place preference, as well as cocaine-induced toxicities. These in vivo studies are described in other chapters in this book and the interested reader is referred to these. Compounds that have dual actions at both σ1 receptors and the dopamine transporter may prove to be a novel strategy for the development of a cocaine-abuse medication and is being investigated toward this goal. Compounds selective at σ2 receptors may be useful as antineoplastic agents or for control of cell survival in neurodegenerative disease. The design and synthesis of novel and selective σ1 and σ2 receptor selective agonists and antagonists will undoubtedly provide the required molecular tools to elucidate both structure and function of these receptors.

Keywords

Conditioned Place Preference Dopamine Transporter Sigma Receptor Sigma Ligand Sigma Receptor Ligand 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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Copyright information

© Springer Science+Business Media, LLC 2007

Authors and Affiliations

  • Amy Hauck Newman
    • 1
  • Andrew Coop
    • 2
  1. 1.Section on Medicinal ChemistryNational Institutes of Health, National Institute on Drug Abuse-Intramural Research ProgramBaltimoreUSA
  2. 2.Department of Pharmaceutical SciencesUniversity of Maryland School of PharmacyBaltimoreUSA

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