4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone: a prejunctional dopamine receptor agonist

J Med Chem. 1985 Oct;28(10):1533-6. doi: 10.1021/jm00148a028.

Abstract

4-[2-(Di-n-propylamino)ethyl]-2(3H)-indolone (1c) (SK&F 101468) is a potent and selective prejunctional dopamine receptor agonist. It caused a dose-related inhibition of the constrictor response to electrical stimulation in the isolated perfused rabbit ear artery (EC50 = 100 nM), and this response was antagonized by (S)-sulpiride (KB = 7 nM). Compound 1c did not stimulate or block dopamine-sensitive adenylate cyclase and did not produce stimulation of the central nervous system in rats. It was prepared from (2-methyl-3-nitrophenyl)acetic acid in a multistep sequence based on the Reissert indole synthesis.

MeSH terms

  • Animals
  • Chemical Phenomena
  • Chemistry
  • Indoles / metabolism
  • Indoles / pharmacology*
  • Rabbits
  • Receptors, Dopamine / drug effects*
  • Vasomotor System / drug effects

Substances

  • Indoles
  • Receptors, Dopamine
  • ropinirole