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

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Fisas MA, Farre A, Camarasa J, Escubedo E

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

Pharmacology. 2004 Oct;72(2):57-67.

PubMed ID
15331910 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Lesopitron5-hydroxytryptamine receptor 1AProteinHumans
Unknown
Not AvailableDetails