Dibenzoazepine analogues: the electrophysiological properties of JL3, a potential atypical antidepressant

Eur J Pharmacol. 1996 Aug 22;310(1):9-12. doi: 10.1016/0014-2999(96)00361-5.

Abstract

JL3, 10-(4-methylpiperazin-1-yl)pyrido[4,3-b][1,4]benzothiazepine, has potent antidepressant-like activity in Porsolt's test in mice. Therefore, its influence on the electrical activity of central monoaminergic neurons was investigated in rats anaesthetized with chloral hydrate. JL3 induced a marked decrease of the firing rate of dorsal raphe serotonergic neurons (ID50 = 3.87 +/- 0.57 mg kg-1) and of locus coeruleus noradrenergic neurons (ID50 = 2.63 +/- 0.35 mg kg-1). The drug did not modify the electrical activity of A10 dopaminergic neurons. JL3 does not block amine uptake but it has affinity for 5-HT1A and 5-HT2 receptors. It is speculated that serotonergic mechanisms could play a role in the electrophysiological effects of JL3.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antidepressive Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Electrophysiology
  • Humans
  • Locus Coeruleus / drug effects
  • Raphe Nuclei / drug effects*
  • Rats
  • Rats, Wistar
  • Thiazepines / pharmacology*

Substances

  • Antidepressive Agents
  • Thiazepines
  • 10-(4-methylpiperazin-1-yl)pyrido(4,3-b)(1,4)benzothiazepine