lesopitron

Lesopitron is a small molecule, non-benzodiazepine anxiolytic that acts as a selective full agonist at the serotonin 5-HT1A receptor. Structurally related to the azapirone class (similar to buspirone), it was developed by Esteve for the treatment of generalized anxiety disorder (GAD). Lesopitron exhibits both pre- and post-synaptic 5-HT1A receptor agonist activity, with negligible effects on alpha-adrenergic and dopaminergic receptors. In animal models, it demonstrated greater potency than other 5-HT1A agonists such as buspirone and showed efficacy in reducing anxiety-like behaviors and countering benzodiazepine withdrawal-induced anxiety. The drug was well tolerated in early clinical trials but development appears to have been discontinued after phase II studies[1][2][3][4][6]. Its mechanism of action involves activation of central serotonin 5-HT1A receptors; it does not affect serotonin reuptake[7]. Lesopitron is rapidly absorbed orally, metabolized hepatically (main metabolite: 5-hydroxylesopitron), with an elimination half-life ranging from about 1.1 to 5.6 hours[3][6].

Other names

lesopitron dihydrochloride