Neurochemical properties of AHR-9377: a novel inhibitor of norepinephrine reuptake

Biochem Pharmacol. 1984 Oct 1;33(19):3001-5. doi: 10.1016/0006-2952(84)90600-2.

Abstract

A novel potential antidepressant, AHR-9377, was evaluated for its inhibition of norepinephrine (NE), serotonin (5-HT) and dopamine (DA) reuptake in hypothalmic, cortical, and striatal rat synaptosomal preparations. AHR-9377 was found to be a potent, selective, noncompetitive inhibitor of NE reuptake. In addition, repeated injections of AHR-9377 caused a decrease in the density of beta adrenergic receptors in rat cerebral cortex. Little displacement by AHR-9377 at beta, alpha 1 and alpha 2 adrenergic, histaminergic, muscarinic, GABA-ergic, benzodiazepine of imipramine sites was observed. These pharmacological properties indicate that AHR-9377 may have clinical antidepressant activity with few side effects.

MeSH terms

  • Animals
  • Antidepressive Agents / pharmacology*
  • Benzodiazepines / pharmacology*
  • Brain / metabolism*
  • Diazepam / metabolism
  • Imipramine / pharmacology
  • In Vitro Techniques
  • Male
  • Norepinephrine / metabolism*
  • Rats
  • Synaptosomes / metabolism
  • Tritium

Substances

  • Antidepressive Agents
  • Tritium
  • Benzodiazepines
  • tampramine fumarate
  • Imipramine
  • Diazepam
  • Norepinephrine