Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia
Lumateperone (2-30 μM) tosylate has anti-tumor activity and can inhibit cell proliferation in a dose-dependent manner. Cell Proliferation Assay Cell Line: RPMI-8226 cells Concentration: 2-30 μM Incubation Time: Result: Inhibited cell growth with the IC50 value of 17.30 μM.
体内研究:
Lumateperone (i.p., 1-10 mg/kg) tosylate promotes NMDA and AMPA-induced currents in a dopamine D 1 receptor-dependent manner and increases the release of dopamine and glutamate in rat mPFC slices. Animal Model: Adult male Sprague-Dawley rats 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.
参考文献:
1. Jinyuan Zhang, et al. Identification of Trovafloxacin, Ozanimod, and Ozenoxacin as Potent c-Myc G-quadruplex Stabilizers to Suppress c-Myc Transcription and Myeloma Growth. Mol Inform. 2022 Mar 30:e2200011. 2. J Titulaer, et al. Lumateperone-mediated effects on prefrontal glutamatergic receptor-mediated neurotransmission: A dopamine D1 receptor dependent mechanism. Eur Neuropsychopharmacol. 2022 Jul 22;62:22-35. 3. Lumateperone