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GABAA receptor
Gamma-
aminobutyric
acid type B
receptor
N-type calcium
channel
potassium
voltage-gated
channel
subfamily J
Adenylate
cyclase type 2
Kappa-type
opioid receptor
Gβ
Gγ
Guanine
nucleotide-
binding protein
G(i) subunit
alpha-1
γ-Aminobutyric acid
Dezocine
cAMP
Ca
+
Ca
+
Na
+
Na
+
γ-Aminobutyric acid
Dezocine
Dezocine
ATP
PP
i
GTP
Pain
Magnesium
More GABA leads to
inhibition of dopamine cell
firing in the spinal cord
pain transmission neurons,
as well as the inhibition of
dopamine cell firing in the
reward system of the brain.
Increased calcium levels
lead to increased
neurotransmitter release.
GABA is released by synaptic
vesicles.
Dezocine antagonizes kappa
opioid receptors in the
spinal cord and the cerebral
cortex
The kappa opioid receptor
through the gamma subunit
inhibits voltage gated
N-type calcium channels,
stopping the influx of
calcium into the neuron
Post-Synaptic Neuron
Pre-Synaptic Neuron
Synapse
Cytosol
Synaptic Vesicle
With the kappa opioid
receptor unable to inhibit
adenylate cyclase, it is
able to synthesize cAMP
which increases the
excitability in spinal cord
pain transmission neurons.
Diffusion
The inhibition of the Gi
subunit of the kappa opioid
receptor prevents the
activation of inwardly
rectifying potassium channel
increasing potassium and
sodium conductance. This
prevents hyperolarization
Kappa opioid inhibition by
Dezocine mainly occurs in
the spinal cord and cerebral
cortex
GABRG2
GABBR1
CACNB1
KCNJ9
ADCY2
OPRK1
GNB1
GNG2
GNAI1
γ-Aminobutyric
acid
Dezocine
cAMP
Calcium
Calcium
Sodium
Sodium
γ-Aminobutyric
acid
Dezocine
Dezocine
Adenosine
triphosphate
Pyrophosphate
Guanosine
triphosphate
Pain
GABRG2
GABBR1
CACNB1
KCNJ9
ADCY2
OPRK1
GNB1
GNG2
GNAI1