Lesopitron

DB04970ExperimentalSmall molecule

Lesopitron is an anxiolytic with pre- and post-synaptic 5-HT1A agonist activity, which is under development by Esteve.

Mechanism: Lesopitron acts as a ligand for central serotonin 5-HT1A receptors. 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.
Curator reviewed
Primary indication: Intended for the treatment of anxiety disorders.Curator reviewed
Formula / weight: C₁₅H₂₁ClN₆ · 320.82 g/mol (avg)
Code names: E-4424

Resolves to

Compound

Structure

InChIKeyAHCPKWJUALHOPH-UHFFFAOYSA-NSMILESClC1=CN(CCCCN2CCN(CC2)C2=NC=CC=N2)N=C1

Targets

What you can answer from here — as of March 06, 2025

1Protein targetEach mapped to UniProt, with action and pharmacological action

Listed above

6+ReferencesStructured and connected to the statements they support

Which drugs share a target with Lesopitron, and which of those have an active Phase 3 trial?

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