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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
CO
2
L-Tyrosine
Tetrahydrobiopterin
O
2
Dihydrobiopterin
H
2
O
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