Effect of prolonged 5-hydroxytryptamine uptake inhibition by paroxetine on cortical beta 1 and beta 2-adrenoceptors in rat brain

Life Sci. 1990;47(18):1683-91. doi: 10.1016/0024-3205(90)90375-2.

Abstract

The effects of prolonged (21 day) oral administration of the antidepressants paroxetine (0.9 to 8.9 mg/kg/day) and amitriptyline (2.7 to 27 mg/kg/day), on rat brain cortical beta 1- and beta 2-adrenoceptor numbers and affinities were investigated using [3H]-CGP 12177. Although amitriptyline, 27 mg/kg, caused a significant (p less than 0.05) 20% reduction in the number of beta 1-adrenoceptors, paroxetine, at doses up to 8.9 mg/kg p.o., did not influence binding of [3H]-CGP 12177 to cortical beta 1- or beta 2-adrenoceptors. This study with paroxetine provides further evidence that the down-regulation of central beta 1-adrenoceptors in rat brain after repeated administration is not a property of all antidepressant drugs.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic beta-Antagonists
  • Amitriptyline / pharmacology
  • Animals
  • Antidepressive Agents / pharmacology*
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism*
  • Dose-Response Relationship, Drug
  • Imidazoles
  • Kinetics
  • Male
  • Neurotransmitter Uptake Inhibitors / pharmacology*
  • Paroxetine
  • Piperidines / pharmacology*
  • Propanolamines
  • Radioligand Assay
  • Rats
  • Receptors, Adrenergic, beta / classification
  • Receptors, Adrenergic, beta / drug effects*
  • Receptors, Serotonin / drug effects
  • Serotonin / physiology*

Substances

  • Adrenergic beta-Antagonists
  • Antidepressive Agents
  • Imidazoles
  • Neurotransmitter Uptake Inhibitors
  • Piperidines
  • Propanolamines
  • Receptors, Adrenergic, beta
  • Receptors, Serotonin
  • Amitriptyline
  • Serotonin
  • Paroxetine
  • CGP 20712A
  • CGP 12177