A comparison of the effects of the selective 5-HT uptake inhibitor WY 27587 on 5-HT uptake into platelets and synaptosomes in the rat

Neuropharmacology. 1989 Jan;28(1):33-6. doi: 10.1016/0028-3908(89)90064-6.

Abstract

N-[( 1-[(6-Fluoro-2-naphthalenyl)methyl]- 4-piperidinyl]amino]carbonyl]-3-pyridine carboxamide (Wy 27587), is 320 times more potent as an inhibitor of the uptake of 5-HT than of the uptake of noradrenaline into synaptosomes from the brain of the rat with a Ki against the uptake of 5-HT of 9.2 +/- 1.4 nM. It was also a potent competitive inhibitor of the uptake of 5-HT in platelets of the rat, with a Ki value of 2.9 +/- 1.5 nM. Ex vivo studies indicated that oral administration of Wy 27587 in the rat caused a prolonged inhibition of the uptake of 5-HT into platelets; inhibition reached a maximum 15 min after administration and the ID50 was 1.5 +/- 0.3 mg/kg.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood Platelets / drug effects*
  • Blood Platelets / metabolism
  • In Vitro Techniques
  • Male
  • Niacinamide / analogs & derivatives*
  • Niacinamide / pharmacology
  • Norepinephrine / metabolism
  • Piperidines / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Serotonin / metabolism*
  • Serotonin Antagonists / pharmacology
  • Synaptosomes / drug effects*
  • Synaptosomes / metabolism

Substances

  • Piperidines
  • Serotonin Antagonists
  • WY 27587
  • Niacinamide
  • Serotonin
  • Norepinephrine