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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+ Brexpiprazole Ca+ Dopamine Dopamine Brexpiprazole Brexpiprazole L-Dopa CO2 L-Tyrosine Tetrahydrobiopterin O2 Dihydrobiopterin H2O Na+ Na+ Pyridoxal 5'-phosphate Gi signaling cascade Fe2+ Cytosol Postsynaptic Neuron Presynaptic Neuron Cytosol Synaptic Vesicle Synapse Norepinephrine is synthesized and stored in synaptic vesicles at the nerve terminal Brexpiprazole is an antagonist at D2 receptor. ↓ Positive, negative and cognitive symptoms of schizophrenia Partial D2 receptor agonism allows Brexpiprazole to stimulate D2 receptors under low dopamine conditions, while attenuating their activation when dopamine levels are high Brain Mesolimbic pathway Blood vessel - blood brain barrier Brexpiprazole is taken orally and absorbed from the gastrointestinal tract. passive diffusion
DRD2 CACNA1A CACNB1 CACNA2D2 SLC6A3 SLC18A2 DDC TH Dopamine Calcium Brexpiprazole Calcium Dopamine Dopamine Brexpiprazole Brexpiprazole L-Dopa Carbon dioxide L-Tyrosine Tetrahydrobiopterin Oxygen Dihydrobiopterin Water Sodium Sodium Gi signaling cascade
DRD2 CACNA1A CACNB1 CACNA2D2 SLC6A3 SLC18A2 DDC TH LDP Ca+ Brexp Ca+ LDP LDP Brexp Brexp L-Dopa CO2 Tyr BH4 O2 BH3 H2O Na+ Na+ Pyr-5'P Gi si c Fe2+ Cytosol Postsynaptic Neuron Presynaptic Neuron Cytosol Synaptic Vesicle Synapse Norepinephrine is synthesized and stored in synaptic vesicles at the nerve terminal Brexpiprazole is an antagonist at D2 receptor. ↓ Positive, negative and cognitive symptoms of schizophrenia Partial D2 receptor agonism allows Brexpiprazole to stimulate D2 receptors under low dopamine conditions, while attenuating their activation when dopamine levels are high Brain Mesolimbic pathway Blood vessel - blood brain barrier Brexpiprazole is taken orally and absorbed from the gastrointestinal tract. passive diffusion
DRD2 CACNA1A CACNB1 CACNA2D2 SLC6A3 SLC18A2 DDC TH LDP Ca2+ Brexp Ca2+ LDP LDP Brexp Brexp L-Dopa CO2 Tyr BH4 O2 BH3 H2O Na+ Na+ Gi si c </