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Gamma-
aminobutyric
acid receptor
subunit beta-2
Gamma-
aminobutyric
acid receptor
subunit gamma-2
Gamma-
aminobutyric
acid type B
receptor
Gamma-
aminobutyric
acid receptor
subunit alpha-1
Adenylate
cyclase type 1
Vesicular
inhibitory
amino acid
transporter
Voltage-
dependent
P/Q-type
calcium channel
subunit
alpha-1A
Multidrug
resistance-
associated
protein 4
Solute carrier
family 22
member 11
Glutamate
decarboxylase 1
3-oxo-5-
alpha-steroid
4-dehydrogenase
1
Aldo-keto
reductase
family 1 member
C4
γ-Aminobutyric acid
cAMP
γ-Aminobutyric acid
Ca
+
Brexanolone
L-Glutamic acid
Cl
-
γ-Aminobutyric acid
Ca
+
Allopregnanolone
Allopregnanolone
Cl
-
CO
2
ATP
PP
i
Progesterone
5a-Pregnane-3,20-dione
Magnesium
Pyridoxal
5'-phosphate
Gi/o signalling
Glutamate
Metabolism
Hyperpolarization
Hyperpolarization leading to
reduced depolarization and
excitability. Decreasing
neuronal excitability has a
sedative effect
Presynaptic Neuron
Post Synaptic Neuron
Synaptic Vesicle
GABA binds to the GABA(a)
receptor in between the
alpha and beta subunits.
Brexanolone
(allopregnanolone) binds to
GABA(A) receptor.
Cytosol
Cytosol
Synapse
Hepatocyte
Endoplasmic Reticulum
5a-reductase converts
progesterone to 5a-DHP.
3a-HSD converts 5a-DHP to
allopregnanolone.
Brexanolone occurs naturally
in the body, but can be
injected intravenously.
Endoplasmic Reticulum
GABRB2
GABRG2
GABBR2
GABRA1
ADCY1
SLC32A1
CACNA1A
ABCC4
SLC22A11
GAD1
SRD5A1
AKR1C4
γ-Aminobutyric
acid
cAMP
γ-Aminobutyric
acid
Calcium
Brexanolone
L-Glutamic acid
Chloride ion
γ-Aminobutyric
acid
Calcium
Allopregnanolone
Allopregnanolone
Chloride ion
Carbon dioxide
Adenosine
triphosphate
Pyrophosphate
Progesterone
5a-Pregnane-
3,20-dione
Gi/o signalling
Glutamate
Metabolism
Hyperpolarization