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D(2) dopamine receptor D(2) dopamine receptor Voltage- dependent P/Q-type calcium channel subunit alpha-1A Voltage- dependent L-type calcium channel subunit beta-1 Voltage- dependent calcium channel subunit alpha-2/delta-2 Sodium- dependent dopamine transporter Synaptic vesicular amine transporter Aromatic-L- amino-acid decarboxylase Tyrosine 3-monooxygenase Dopamine Ca+ Lumateperone Ca+ Dopamine Dopamine Lumateperone Lumateperone L-Dopa CO2 L-Tyrosine Tetrahydrobiopterin O2 Dihydrobiopterin H2O Na+ Pyridoxal 5'-phosphate Na+ Gi signaling cascade Fe2+ Cytosol Postsynaptic Neuron Presynaptic Neuron Cytosol Synaptic Vesicle Synapse Lumateperone is a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors. ↓ Positive, negative and cognitive symptoms of psychosis Lumateperone efficiently reduces dopamine signaling Brain Mesolimbic pathway Blood vessel - blood brain barrier Lumateperone is taken orally and absorbed from the gastrointestinal tract passive diffusion Partial D2 receptor agonism allows lumateperone to stimulate D2 receptors under low dopamine conditions, while attenuating their activation when dopamine levels are high.
DRD2 DRD2 CACNA1A CACNB1 CACNA2D2 SLC6A3 SLC18A2 DDC TH Dopamine Calcium Lumateperone Calcium Dopamine Dopamine Lumateperone Lumateperone L-Dopa Carbon dioxide L-Tyrosine Tetrahydrobiopterin Oxygen Dihydrobiopterin Water Sodium Sodium Gi signaling cascade
DRD2 DRD2 CACNA1A CACNB1 CACNA2D2 SLC6A3 SLC18A2 DDC TH LDP Ca+ Lumat Ca+ LDP LDP Lumat Lumat L-Dopa CO2 Tyr BH4 O2 BH3 H2O Na+ Pyr-5'P Na+ Gi si c Fe2+ Cytosol Postsynaptic Neuron Presynaptic Neuron Cytosol Synaptic Vesicle Synapse Lumateperone is a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors. ↓ Positive, negative and cognitive symptoms of psychosis Lumateperone efficiently reduces dopamine signaling Brain Mesolimbic pathway Blood vessel - blood brain barrier Lumateperone is taken orally and absorbed from the gastrointestinal tract passive diffusion Partial D2 receptor agonism allows lumateperone to stimulate D2 receptors under low dopamine conditions, while attenuating their activation when dopamine levels are high.