Synthesis and dopamine receptor affinities of 6-amino-5,6,7,8-tetrahydroquinoline derivatives

Drug Des Deliv. 1989 Jun;4(4):279-87.

Abstract

Some N,N-dialkylderivatives of 6-amino-5,6,7,8-tetrahydroquinoline were synthesized. The affinity of new compounds for dopamine binding sites was measured in a test involving displacement of [3H]SCH 23390 (D-1 selective) and [3H]spiperone (D-2 selective) from homogenized rat striatal tissue. While no compound was effective in displacing [3H]SCH 23390, in the binding assays on the D-2 receptor all tetrahydroquinolines displaced [3H]spiperone from specific binding sites, the compounds with a N-n-propyl-N-phenylethylamino group (18) or N,N-di n-propylamino group (16) being the most potent.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine
  • Aminoquinolines / chemical synthesis
  • Aminoquinolines / pharmacology*
  • Animals
  • Benzazepines / pharmacology
  • Binding, Competitive / drug effects
  • Chemical Phenomena
  • Chemistry
  • Corpus Striatum / drug effects
  • Corpus Striatum / metabolism
  • Dopamine Agents / pharmacology
  • In Vitro Techniques
  • Rats
  • Rats, Inbred Strains
  • Receptors, Dopamine / drug effects*

Substances

  • Aminoquinolines
  • Benzazepines
  • Dopamine Agents
  • Receptors, Dopamine
  • 2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine