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5- hydroxytryptamine receptor 2A 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 Synaptic vesicular amine transporter Sodium- dependent serotonin transporter Solute carrier family 22 member 1 Solute carrier family 22 member 1 Tryptophan 5-hydroxylase 1 Aromatic-L- amino-acid decarboxylase Cytochrome P450 2D6 Ca+ Serotonin Serotonin Paliperidone Risperidone Ca+ Serotonin Paliperidone Risperidone Risperidone Risperidone L-Tryptophan Tetrahydrobiopterin O2 5-Hydroxy-L-tryptophan 4a-Hydroxytetrahydrobiopterin CO2 Paliperidone Na+ Na+ Fe2+ Pyridoxal 5'-phosphate Heme Gq signaling cascade Synaptic Vesicle Cytosol Cytosol Presynaptic Neuron Postsynaptic Neuron Synapse ↓ Negative symptoms of schizophrenia Serotonin is synthesized and stored in synaptic vesicles at the nerve terminal Risperidone binds to 5HT2A where it acts as a functional antagonist to reduce negative symptoms of schizophrenia ↑Cognitive Improvement Brain Raphei nuclei producing serotonergic neurons Blood vessel -blood brain barrier Passive Diffusion Risperidone also acts as an antagonist to Dopamine D1, D2, Alpha 1A and 1B receptors Risperidone is taken orally and absorbed from the gastrointestinal tract. hepatocytes Liver endoplasmic reticulum Risperidone is converted to a major active metabolite, 9 -hydroxyrisperidone Risperidone and its active metabolite, 9 -hydroxyrisperidone - paliperidone are often regarded as equipotent. Mesolimbic pathway
Endoplasmic Reticulum HTR2A CACNA1A CACNB1 CACNA2D2 SLC18A2 SLC6A4 SLC22A1 SLC22A1 TPH1 DDC CYP2D6 Calcium Serotonin Serotonin Paliperidone Risperidone Calcium Serotonin Paliperidone Risperidone Risperidone Risperidone L-Tryptophan Tetrahydrobiopterin Oxygen 5-Hydroxy-L- tryptophan 4a- Hydroxytetrahydrobiopterin Carbon dioxide Paliperidone Sodium Sodium Gq signaling cascade