Journal of Medicinal Chemistry p. 1533 - 1536 (1985)
Update date:2022-08-03
Topics:
Gallagher, Gregory
Lavanchy, Patricia G.
Wilson, James W.
Hieble, J. Paul
DeMarinis, Robert M.
4-<2-(Di-n-propylamino)ethyl>-2(3H)-indolone (1c) (SK and 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.
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