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5-
hydroxytryptamine
receptor 1A
Sodium-
dependent
serotonin
transporter
D(1A) dopamine
receptor
Sodium-
dependent
dopamine
transporter
Alpha-1A
adrenergic
receptor
Synaptic
vesicular amine
transporter
Synaptic
vesicular amine
transporter
Synaptic
vesicular amine
transporter
Tryptophan
5-hydroxylase 1
Aromatic-L-
amino-acid
decarboxylase
Tyrosine
3-monooxygenase
Aromatic-L-
amino-acid
decarboxylase
Dopamine beta-
hydroxylase
Sodium-
dependent
noradrenaline
transporter
Serotonin
Venlafaxine
Dopamine
Serotonin
Serotonin
Serotonin
Na+
Na+
Dopamine
Dopamine
Norepinephrine
Norepinephrine
L-Tryptophan
Tetrahydrobiopterin
O2
5-Hydroxy-L-
tryptophan
4a-
Hydroxytetrahydrobiopterin
CO2
L-Tyrosine
L-Dopa
CO2
Ascorbic acid
O2
Norepinephrine
Dehydroascorbic
acid
H2 O
Na+
Dopamine
Na+
Norepinephrine
Na+
Na+
Fe2+
Pyridoxal
5'-phosphate
Fe2+
Pyridoxal
5'-phosphate
Pyrroloquinoline
quinone
Copper
Venlafaxine transport in and
out of the blood-brain
barrier involves the
multidrug resistance protein
1 (an ATP-binding cassette
sub-family G member 2).
Presynaptic cell
Synaptic Cleft
Post synaptic cell
Synaptic Vesicle
Cytosol
Venlafaxine is a selective
serotonin and norepinephrine
(AKA noradrenaline, NA)
reuptake inhibitor (SSNRI)
which binds to the sodium
dependent serotonin and NA
transporters present
throughout the central
nervous system, allowing
serotonin and NA to
accumulate in the synaptic
cleft, which significantly
enhances serotonergic
activity and increases
adrenergic signaling in the
brain. It appears to
similarly act on dopamine
receptors, prolonging
dopaminergic effects in the
synaptic cleft, though this
effect is not majorly
implicated in the mechanism
of action, along with
potential effects on other
neurotransmitters.
Serotonin that accumulates
in the synaptic cleft binds
to the 5-HT 1A receptors.
5-HT 1A receptors are
responsible for lower
anxiety and antidepressant
effects.
Dopamine accumulates in the
cleft and can bind to
various dopamine receptors.
Shown here is the dopamine
1A receptor, a common
Gs-coupled target in
treating depression.
Norepinephrine is another
monoamine that accumulates
in the cleft as a result of
venlafaxine's inhibitory
action. Norepinephrine can
act on many adrenergic
receptors in the nervous
system (here, the α-1A
receptor is shown, which is
also a common antipsychotic
target) to aid in
anti-depressive signaling.
HTR1A
SLC6A4
DRD1
SLC6A3
ADRA1A
SLC18A2
SLC18A2
SLC18A2
TPH1
DDC
TH
DDC
DBH
SLC6A2
Serotonin
Venlafaxine
Dopamine
Serotonin
Serotonin
Serotonin
Sodium
Sodium
Dopamine
Dopamine
Norepinephrine
Norepinephrine
L-Tryptophan
Tetrahydrobiopterin
Oxygen
5-Hydroxy-L-
tryptophan
4a-
Hydroxytetrahydrobiopterin
Carbon dioxide
L-Tyrosine
L-Dopa
Carbon dioxide
Ascorbic acid
Oxygen
Norepinephrine
Dehydroascorbic
acid
Water
Sodium
Dopamine
Sodium
Norepinephrine
Sodium
Sodium
HTR1A
SLC6A4
DRD1
SLC6A3
ADRA1A
SLC18A2
SLC18A2
SLC18A2
TPH1
DDC
TH
DDC
DBH
SLC6A2
5-HT
Venlafa
LDP
5-HT
5-HT
5-HT
Na+
Na+
LDP
LDP
Norpp
Norpp
Trp
BH4
O2
5-HTP
4aHtHbp
CO2
Tyr
L-Dopa
CO2
VitC
O2
Norpp
DHAA
H2 O
Na+
LDP
Na+
Norpp
Na+
Na+
Fe2+
Pyr-5'P
Fe2+
Pyr-5'P
Pqq
Cu
Venlafaxine transport in and
out of the blood-brain
barrier involves the
multidrug resistance protein
1 (an ATP-binding cassette
sub-family G member 2).
Presynaptic cell
Synaptic Cleft
Post synaptic cell
Synaptic Vesicle
Cytosol
Venlafaxine is a selective
serotonin and norepinephrine
(AKA noradrenaline, NA)
reuptake inhibitor (SSNRI)
which binds to the sodium
dependent serotonin and NA
transporters present
throughout the central
nervous system, allowing
serotonin and NA to
accumulate in the synaptic
cleft, which significantly
enhances serotonergic
activity and increases
adrenergic signaling in the
brain. It appears to
similarly act on dopamine
receptors, prolonging
dopaminergic effects in the
synaptic cleft, though this
effect is not majorly
implicated in the mechanism
of action, along with
potential effects on other
neurotransmitters.
Serotonin that accumulates
in the synaptic cleft binds
to the 5-HT 1A receptors.
5-HT 1A receptors are
responsible for lower
anxiety and antidepressant
effects.
Dopamine accumulates in the
cleft and can bind to
various dopamine receptors.
Shown here is the dopamine
1A receptor, a common
Gs-coupled target in
treating depression.
Norepinephrine is another
monoamine that accumulates
in the cleft as a result of
venlafaxine's inhibitory
action. Norepinephrine can
act on many adrenergic
receptors in the nervous
system (here, the α-1A
receptor is shown, which is
also a common antipsychotic
target) to aid in
anti-depressive signaling.
HTR1A
SLC6A4
DRD1
SLC6A3
ADRA1A
SLC18A2
SLC18A2
SLC18A2
TPH1
DDC
TH
DDC
DBH
SLC6A2
5-HT
Venlafa
LDP
5-HT
5-HT
5-HT
Na+
Na+
LDP
LDP
Norpp
Norpp
Trp
BH4
O2
5-HTP
4aHtHbp
CO2
Tyr
L-Dopa
CO2
VitC
O2
Norpp
DHAA
H2O
Na+
LDP
Na+
Norpp
Na+
Na+