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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 Solute carrier family 22 member 1 Solute carrier family 22 member 1 Aromatic-L- amino-acid decarboxylase Tyrosine 3-monooxygenase Cytochrome P450 2D6 Dopamine Ca+ Paliperidone Risperidone Ca+ Dopamine Dopamine Paliperidone Risperidone Risperidone Risperidone L-Dopa CO2 L-Tyrosine Tetrahydrobiopterin O2 Dihydrobiopterin H2O Paliperidone Na+ Na+ Pyridoxal 5'-phosphate Heme Gi signaling cascade Fe2+ Cytosol Postsynaptic Neuron Presynaptic Neuron Cytosol Synaptic Vesicle Synapse Paliperidone is an active metabolite of risperidone and a D2 receptor antagonist. ↓ Positive, negative and cognitive symptoms of schizophrenia Excess dopamine in the brain triggers positive symptoms of schizophrenia Brain Mesolimbic pathway Blood vessel - blood brain barrier Passive Diffusion 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.
Endoplasmic Reticulum DRD2 CACNA1A CACNB1 CACNA2D2 SLC6A3 SLC18A2 SLC22A1 SLC22A1 DDC TH CYP2D6 Dopamine Calcium Paliperidone Risperidone Calcium Dopamine Dopamine Paliperidone Risperidone Risperidone Risperidone L-Dopa Carbon dioxide L-Tyrosine Tetrahydrobiopterin Oxygen Dihydrobiopterin Water Paliperidone Sodium Sodium Gi signaling cascade