Synthesis and neuropharmacological evaluation of 2-aryl- and alkylapomorphines

Bioorg Med Chem. 2008 Apr 1;16(7):3773-9. doi: 10.1016/j.bmc.2008.01.057. Epub 2008 Feb 5.

Abstract

A novel synthesis has been elaborated for the pharmacologically remarkable 2-arylapomorphines described and characterized in the last few years. This new procedure contains two alternative synthetic routes and has allowed the preparation of several hitherto unknown compounds as well. The pharmacological profile of the previously published and the novel 2-alkyl- and arylapomorphines has been determined with the application of in vitro and in vivo techniques. For 2-phenyl- (2) and 2-(4-hydroxyphenyl)apomorphines (3) the superior dopamine agonist profile has been confirmed and for the novel compounds some remarkable results have been observed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Animals
  • Apomorphine / chemical synthesis*
  • Apomorphine / chemistry
  • Apomorphine / pharmacology*
  • Cell Line
  • Male
  • Mice
  • Molecular Structure
  • Neurons / drug effects*
  • Spodoptera
  • Structure-Activity Relationship

Substances

  • Apomorphine