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

Citations Over TimeTop 24% of 1985 papers

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.

Related Papers

• → Estimation of partial agonist affinity by interaction with a full agonist: a direct operational model‐fitting approach(1993)48 cited
• → Different structures of the two peroxisome proliferator-activated receptor gamma (PPARγ) ligand-binding domains in homodimeric complex with partial agonist, but not full agonist(2015)16 cited
• → Induction of the Early Growth Response Gene 1 Promoter by TCR Agonists and Partial Agonists: Ligand Potency Is Related to Sustained Phosphorylation of Extracellular Signal-Related Kinase Substrates(2003)23 cited
• → Predicting the Activation of the Androgen Receptor by Mixtures of Ligands Using Generalized Concentration Addition(2020)6 cited
• → Human fat cell alpha-2 adrenoceptors. II. Comparative study of partial and full agonist binding parameters using [3H]clonidine and [3H]UK-14,304.(1989)12 cited