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Myosin light
chain kinase,
smooth muscle
5-
hydroxytryptamine
receptor 1B
Guanine
nucleotide-
binding protein
G(i) subunit
alpha-1
Guanine
nucleotide-
binding protein
G(I)/G(S)/G(T)
subunit beta-1
Gγ
Adenylate
cyclase type 5
PKA complex
PKA complex
Myosin LC-P
Myosin light
chain 3
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
Serine/threonine-
protein
phosphatase
PP1-beta
catalytic
subunit
Calmodulin-1
Calmodulin-1
cAMP
Eletriptan
Ca
+
Ca
+
ATP
ATP
PP
i
Ca
+
Muscle
Contraction
Muscle
Relaxation
Vasoconstriction
Magnesium
Calcium
Manganese
Myosin binds from actin
causing the sarcomere
filaments to slide leading
to smooth muscle contraction
and vasoconstriction
Increased calcium binds
readily to calmodulin to
activate myosin light chain
kinase
Reduced protein kinase A
(PKA) activity is generally
associated with increased
intracellular calcium
concentration and the
activation of myosin light
chain kinase (MLCK), all of
which contribute to smooth
muscle contraction and blood
vessel constriction.
Cytosol
Activation of myosin light
chain kinase leads to high
concentration of myosin LC-P
which causes contractions of
the muscles
Vascular Smooth Muscle Cell
Constriction
Eletriptan is an agonist at
5-HT1B, 1D, 1F receptors
present on smooth muscles
within the blood vessels and
peripheral terminals of the
trigeminal nerve innervating
cranial blood vessels
Actin Filament
Myosin Filament
Eletriptan is administered
as an oral pill
Lower PKA activity leads to
decreased phosphorylation of
certain proteins, including
myosin light chain (MLC), in
smooth muscle cells. Reduced
MLC phosphorylation promotes
the activation of myosin
light chain kinase (MLCK).
Decreased cAMP levels can
lead to increased
intracellular calcium
concentration by various
mechanisms, including the
release of calcium from
intracellular stores.
Eletriptan decreases carotid
arterial blood flow, but
increases blood flow
velocity in the internal
carotid artery and middle
cerebral artery
Cranial blood vessels
Brain
MYLK
HTR1B
GNAI1
GNB1
GNG2
ADCY5
PRKAR1A
PRKAR2A
MYL3
MYL3
CACNA1A
CACNB1
CACNA2D2
PPP1CB
CALM1
CALM1
cAMP
Eletriptan
Calcium
Calcium
Adenosine
triphosphate
Adenosine
triphosphate
Pyrophosphate
Calcium
Muscle
Contraction
Muscle
Relaxation
Vasoconstriction