5-HT and benzodiazepine receptor ligands. III. Synthesis and receptor affinities of 1,2,4-triazolo[4',3':1,6]pyridazino[4,5-b]quinoline and 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinoline-1-one derivatives

Farmaco. 1990 Nov;45(11):1169-79.

Abstract

The syntheses as well as 5-HT and Benzodiazepine receptor binding studies of some 1,2,4-Triazolo[4',3':1,6]piridazino[4,5-b]quinoline and 2,3-Dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinoline-1-one derivatives are reported. While the triazole-containing heterocycles are devoid of any biological activity, 2-benzyl-2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinoline-1-one shows some affinity for the central type of benzodiazepine receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive / drug effects
  • Brain / drug effects
  • Brain / metabolism
  • Cerebellum / drug effects
  • Cerebellum / metabolism
  • Flumazenil / metabolism
  • In Vitro Techniques
  • Isoquinolines / metabolism
  • Ligands
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Quinolones / chemical synthesis*
  • Quinolones / pharmacology
  • Rats
  • Receptors, GABA-A / drug effects*
  • Receptors, Serotonin / drug effects*

Substances

  • Isoquinolines
  • Ligands
  • Pyrroles
  • Quinolones
  • Receptors, GABA-A
  • Receptors, Serotonin
  • Flumazenil
  • PK 11195