25 Vascular tone regulation Flashcards
________ is a Ca2+-binding protein to form a complex
which regulates smooth muscle contraction and
many other cellular functions.
Calmodulin
Ca2+/calmodulin will cause phosphorylation of ___________ by ___________. It results in smooth muscle __________.
Myosin light chain
Myosin light chain kinase
contraction
_________ will convert MLC-P + actin into MCL, causing smooth muscle relaxation.
Myosin light chain phosphatase
Noradrenaline, AngII, endothelin and vasopressin are coupled to _________ protein. What are the following reactions?
______ on SR is also activated
Gq
PLC causes PIP2 > IP3
IP3 + DAG > release intracellular Ca2+ from sarcoplasmic reticulum
Ryanodine receptors
To inhibit Ca2+ influx via voltage-gated Ca2+ channel, we can use L-type channel blockers.
List 3 examples.
Dihydropyridines (nifedipine)
Phenylalkylamines (verapamil)
Benzothiazepines (diltiazem)
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Ca2+ channel blockers are used clinically in ?
Controlling hypertension by reducing vascular resistance
What are the 4 main [Ca2+i] lowering mechanisms?
- SERCA Ca2+ pump, uptake Ca2+ ions to SR
- Plasma Ca2+ pump to remove part of the increased intracellular Ca2+ ions
- Closure of voltage gated Ca2+ channels by membrane hyperpolarization from opening of K+ channels
- Na+/Ca2+ exchanger (3 Na+ in, 1 Ca2+ out)
Defective ______ channels have been implicated in pulmonary hypertension.
K+
Reduced in K+ channel activity tends to cause depolarization and subsequent activation of Ca2+ channels that increases intracellular [Ca2+]
What do beta 2 agonist, VIP and adenosine do in vascular tone?
bind to endothelial cells Gs protein, increase cAMP by stimulating AC, thus PKA increases. Hyperpolarization occurs, reduce intracellular Ca2+. Vasodilation.
What do noradrenaline, endothelin 1 and angiotensin II do in vascular tone?
they bind to a1 receptors can activate Gq protein. Increase in PLC, converting PIP2 to IP3, + DAG > increase SR Ca2+ release> vasoconstriction
What are the 3 vasoconstrictors that are hormones in nature?
Angiontensin II, vasopressin, endothelin
What are the 3 vasodilators that are hormone in nature?
- CGRP (Calcitonin gene-related peptide)
- Atrial natriuretic peptide (ANP)
- VIP (vasoactive intestinal polypeptide)