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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
Tryptophan
5-hydroxylase 1
Aromatic-L-
amino-acid
decarboxylase
Ca
+
Serotonin
Serotonin
Dosulepin
Ca
+
Serotonin
Dosulepin
Dosulepin
L-Tryptophan
Tetrahydrobiopterin
O
2
5-Hydroxy-L-tryptophan
4a-Hydroxytetrahydrobiopterin
CO
2
Na
+
Na
+
Fe2+
Pyridoxal
5'-phosphate
Gq signaling
cascade
Synaptic Vesicle
Cytosol
Cytosol
Presynaptic Neuron
Postsynaptic Neuron
Synapse
↓ depressive and anxiolytic
symptoms
Serotonin is synthesized at
the raphei nuclei and stored
in synaptic vesicles at the
nerve terminal
Dosulepin binds to 5HT1A and
5HT2A where it exhibits
antidepressive and
anxiolytic properties
Brain
Raphei nuclei producing
serotonergic neurons
Blood vessel -blood brain
barrier
passive diffusion
Dosulepin is administered
orally
Dosulepin also acts as an
antagonist to D2, M1 and H1
receptors.
HTR2A
CACNA1A
CACNB1
CACNA2D2
SLC18A2
SLC6A4
TPH1
DDC
Calcium
Serotonin
Serotonin
Dosulepin
Calcium
Serotonin
Dosulepin
Dosulepin
L-Tryptophan
Tetrahydrobiopterin
Oxygen
5-Hydroxy-L-
tryptophan
4a-
Hydroxytetrahydrobiopterin
Carbon dioxide
Sodium
Sodium
Gq signaling
cascade
HTR2A
CACNA1A
CACNB1
CACNA2D2
SLC18A2
SLC6A4
TPH1
DDC
Ca
+
5-HT
5-HT
Dosul
Ca
+
5-HT
Dosul
Dosul
Trp
BH4
O
2
5-HTP
4aHtHbp
CO
2
Na
+
Na
+
Fe2+
Pyr-5'P
Gq si c
Synaptic Vesicle
Cytosol
Cytosol
Presynaptic Neuron
Postsynaptic Neuron
Synapse
↓ depressive and anxiolytic
symptoms
Serotonin is synthesized at
the raphei nuclei and stored
in synaptic vesicles at the
nerve terminal
Dosulepin binds to 5HT1A and
5HT2A where it exhibits
antidepressive and
anxiolytic properties
Brain
Raphei nuclei producing
serotonergic neurons
Blood vessel -blood brain
barrier
passive diffusion
Dosulepin is administered
orally
Dosulepin also acts as an
antagonist to D2, M1 and H1
receptors.