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Effects of lesopitron on the central nervous system arising from its interaction with 5-HT1A receptors.

Abstract
Lesopitron acts as a ligand for central serotonin 5-HT1A receptors. Ki obtained from [3H]8-OH-DPAT competition studies was 104.8 +/- 10.6 nmol/l. As lesopitron did not affect the binding of [3H]paroxetine, involvement of the serotonin reuptake system in the effects of lesopitron is rejected. Lesopitron inhibits haloperidol-induced catalepsy that is the consequence of its action on 5-HT1A autoreceptors. The ability of lesopitron to induce 5-HT syndrome reflects post-synaptic 5-HT1A receptor activation and the reversion of 8-OHDPAT-induced 5-HT syndrome by lesopitron suggests a partial agonist effect on this receptor-type. Lesopitron induced a hypothermic effect due to the enhanced activation of post-synaptic 5-HT1A receptors. The agonist effect of lesopitron on 5-HT1A receptors and its marked hypothermic effect is an added value for this drug and a stimulus to the study of its possible neuroprotective action.
AuthorsM Angels Fisas, Antonio Farré, Jorge Camarasa, Elena Escubedo
JournalPharmacology (Pharmacology) Vol. 72 Issue 2 Pg. 57-67 (Oct 2004) ISSN: 0031-7012 [Print] Switzerland
PMID15331910 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Central Nervous System Depressants
  • Ligands
  • Piperazines
  • Pyrimidines
  • Serotonin 5-HT1 Receptor Agonists
  • Serotonin Uptake Inhibitors
  • Paroxetine
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • lesopitron
Topics
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Animals
  • Catalepsy (chemically induced)
  • Central Nervous System (drug effects)
  • Central Nervous System Depressants (pharmacology)
  • Drug Interactions
  • Female
  • Hippocampus (metabolism)
  • Hypothermia (chemically induced)
  • In Vitro Techniques
  • Ligands
  • Male
  • Mice
  • Paroxetine (pharmacology)
  • Piperazines (pharmacology)
  • Pyrimidines (pharmacology)
  • Radioligand Assay
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Serotonin 5-HT1 Receptor Agonists
  • Serotonin Syndrome (chemically induced)
  • Selective Serotonin Reuptake Inhibitors (pharmacology)
  • Species Specificity

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