Lumateperone is a novel antipsychotic agent with a unique mechanism of
action with high 5-hydroxytryptamine 2A(5-HT2A) blocking activity. A
Phase 2 study in treatment of insomnia revealed strong evidence of
efficacy, with no impairment of next-day cognition.
Lumateperone was a drug developed for the treatment of schizophrenia. May have applications in bipolar depression.
Synthesis of Lumateperone

Lumateperone (i.p., 1-10 mg/kg) promotes NMDA and AMPA-induced currents in a dopamine D1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices[2].
| Animal Model: | Adult male Sprague-Dawley rats[2] |
| Dosage: | 1-10 mg/kg |
| Administration: | Intraperitoneal injection |
| Result: | Inhibited avoidance response at concentrations of 1, 3 and 10 mg/kg after 20 minutes.
Promoted NMDA and AMPA-sensitive currents, also significantly increased dopamine and glutamate release at 10 mg/kg in mPFC cone cells of rat.
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[1] Patent: US2004/220178, 2004, A1