A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol

Bioorg Med Chem. 2008 Mar 15;16(6):3438-44. doi: 10.1016/j.bmc.2007.06.036. Epub 2007 Jun 23.

Abstract

Previously, we have demonstrated that enone prodrugs of dopaminergic catecholamines represent a new type of dopamine (DA) agonist. Trans-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol (TL-334), the active form of trans-1-propyl-2,3,4,4a,5,7,8,9,10,10a-decahydro-1H-benzo[g]quinolin-6-one (GMC-6650), in vivo showed an extremely potent dopaminergic activity. Here, we report a novel synthesis and a pharmacological evaluation of TL-334 by means of microdialysis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Brain Chemistry
  • Cell Line
  • Dialysis
  • Dopamine Agonists / chemical synthesis
  • Humans
  • Microchemistry / methods
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Receptors, Dopamine D1 / agonists*
  • Receptors, Dopamine D2 / agonists*
  • Transfection

Substances

  • Dopamine Agonists
  • Quinolines
  • Receptors, Dopamine D1
  • Receptors, Dopamine D2