Alaproclate: further pharmacological evidence for 5-HT uptake inhibition in vivo

Arch Int Pharmacodyn Ther. 1983 Oct;265(2):219-29.

Abstract

Alaproclate (2-/4-chlorophenyl/-1,1-dimethyl-2-amino-propanoate hydrochloride), a new selective 5-HT uptake inhibitor has been studied for its in vivo effects on the 5-HT transmission in rats in the following tests: 1) the flexor reflex in the spinal rat, 2) hyperthermia in rats at a high ambient temperature, 3) rat stomach fundus strip preparation. Alaproclate prevented potentiation of the flexor reflex in spinal rats induced by 5-HT releasers fenfluramine and p-chloroamphetamine (PCA) but did not affect the potentiation of the reflex due to direct 5-HT agonists LSD and quipazine. Also hyperthermic response of rats to fenfluramine was antagonized by alaproclate, whereas that due to quipazine was potentiated. Alaproclate failed to inhibit 5-HT-induced contractile response in rat stomach fundus strip preparation. The results confirm in vivo 5-HT uptake inhibition by alaproclate in the central nervous system, and its lack of blocking effect on postsynaptic 5-HT receptors.

MeSH terms

  • Alanine / analogs & derivatives*
  • Alanine / pharmacology
  • Animals
  • Central Nervous System / metabolism*
  • Male
  • Muscle Contraction / drug effects
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / drug effects*
  • Reflex / drug effects
  • Serotonin / metabolism*
  • Stomach / physiology

Substances

  • Receptors, Serotonin
  • Serotonin
  • alaproclate
  • Alanine