Central monoaminergic effects of two aporphine analogues to the putative serotonin-receptor agonist, 8-hydroxy-2-di-n-propylaminotetralin

Neuropharmacology. 1984 Oct;23(10):1187-90. doi: 10.1016/0028-3908(84)90237-5.

Abstract

Two aporphine analogues to the potent and selective serotonin (5-HT) agonist, 8-hydroxy-2-di-n-propylaminotetralin (8-OH-DPAT) were studied with regard to their actions upon central monoaminergic systems. The biochemical and behavioural findings indicate that 8-hydroxy-N-methyl-aporphine (8-OH aporphine) and its N-n-propyl analogue (8-OH PNA) possess weak dopamine/noradrenaline antagonist- and agonist-like properties, respectively. In addition, both aporphines seemed to only weakly influence serotoninergic transmission. The latter findings are compared to those of known serotonin agonists (e.g. 8-OH-DPAT), and are discussed with particular reference to the structural requirements for activation of central 5-HT receptors.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Aporphines / pharmacology*
  • Biogenic Amines / physiology*
  • Brain / drug effects*
  • Dopamine / physiology
  • Male
  • Norepinephrine / physiology
  • Rats
  • Rats, Inbred Strains
  • Serotonin / physiology
  • Structure-Activity Relationship
  • Synaptic Transmission / drug effects*

Substances

  • Aporphines
  • Biogenic Amines
  • Serotonin
  • 8-hydroxy-N-n-propylnoraporphine
  • 8-hydroxy-N-methylaporphine
  • Dopamine
  • Norepinephrine