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.
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Authors | M Angels Fisas, Antonio Farré, Jorge Camarasa, Elena Escubedo |
Journal | Pharmacology
(Pharmacology)
Vol. 72
Issue 2
Pg. 57-67
(Oct 2004)
ISSN: 0031-7012 [Print] Switzerland |
PMID | 15331910
(Publication Type: Comparative Study, Journal Article)
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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
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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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