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Re: What does Lumateperone do to dopamine receptors?

Posted by greg rizzo on January 9, 2020, at 20:42:15

In reply to Re: What does Lumateperone do to dopamine receptors? Lamdage22, posted by undopaminergic on December 24, 2019, at 7:49:42

jUST SOME BABBLE FROM THE NET. mY IMPRESSION IS THAT IT IS MAINLY INTENDED FOR SCHITZOPHREIA, BUT YES DOES INCREASE DOPAMINE. WHAT DOSAGE? UNSURE
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Intra-Cellular Therapies announced early Monday morning lumateperone (CAPLYTA) had received approval from the FDA and the company expects the treatment to be available in late Q1 2020.
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Mechanism of action
Lumateperone affects multiple systems (serotonergic, dopaminergic and glutamatergic) in the central nervous system. It acts as a antagonist of 5HT2A 0.54nM receptor and modulates D1 4.1nM and D2 3.2nM dopamine receptors where it is a partial agonist at presynaptic and antagonist at postsynaptic receptors. Serotonin transporters at 3.3nM. Through the mTOR pathway, lumateperone aguments both NMDA and AMPA activity. Because of its complex pharmacology, it is not clear which of these activities are primarily responsible for its antidepressive and antipsychotic activities.[14]
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. With approximately 2.4 million adults with schizophrenia in the United States, the potent serotonin 5-HT2A receptor antagonist, a DPPM acting as a presynaptic partial agonist and postsynaptic antagonist at dopamine D2 receptors, a dopamine D1 receptor-dependent indirect modulator of glutamate, and a serotonin reuptake inhibitor represents a new option to meet the ongoing unmet need for treatments.
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Lumateperone is a newly approved 2nd generation antipsychotic currently indicated for the treatment of schizophrenia.1 It has a unique receptor binding profile and differs from other antipsychotics in that it modulates glutamate, serotonin and dopamine, which are all neurotransmitters that contribute to the pathophysiology of schizophrenia.1,5

The data so far indicates that lumateperone can alleviate both positive and negative symptoms of schizophrenia.1 Further, not only is the new antipsychotic selective for dopamine (D2) receptors in the mesolimbic and mesocortical brain regions, but it also has minimal off-target activity


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poster:greg rizzo thread:1096899
URL: http://www.dr-bob.org/babble/20200104/msgs/1107768.html