Synthesis and Structure-Activity Relationships of 3-Arylalkylbenz-Isoindolines: Novel Potential Antidepressants
Abstract
A series of 3-arylalkyl-benz[ e]isoindolines 1 was synthesized and examined for inhibition of biogenic amine uptake, which in the past has been predictive of antidepressant activity. We have identified inhibitors of the reuptake of norepinephrine (NE), dopamine (DA), and serotonin (5HT) in synaptosomal preparations from rat hypothalamus, striatum and cortex respectively. Most of the compounds inhibit NE reuptake more potently than DA reuptake, and their activity at inhibiting 5HT reuptake is considerably weaker.
Fields of Study & Subjects
Synthesis and pharmacology of benzodiazepine derivatives
Neurotransmitter Receptor Influence on Behavior
Cyclization and Aryne Chemistry
Publication details
- Pages
- 239–248
- Publication date
- 8 January 2026
- Language
- EN
- Document type
- Book chapter