Regulation of the Cardiovascular System Flashcards
7-transmembrane-spanning integral membrane proteins
Extremely important for intracellular signaling throughout body
G protein-coupled receptors (GPCRs)
used to treat arrhythmias, hypertension, and for cardioprotection post-MI
many subtypes
b blockers
GPCRs are the most prevalent drug target!
used to treat hypertension and heart failure
angiotensin II receptor blockers
GPCRs are the most prevalent drug target!
stimulatory G protein
activates adenylate cyclase
ncreases cAMP, activates PIKA
Gs
inhibitory G protein
inhibits adenylate cyclase
Decreases cAMP, inhibits PKA
Gi/o
activates PLC and PKC
Increases Ca2+ (via IP3R activation & SR Ca2+ release)
Gq
Sympathetic stimulation increases inotropy
Little parasympathetic regulation of ______
inotropy
Sympathetic stimulation increases inotropy via ________ of 4 proteins involved in EC coupling.
PKA phosphorylation
relieves inhibition of SERCA
faster Ca2+ reuptake into SR.
Increases lusitropy.
Increases inotropy by increasing SR Ca2+ load.
PKA phosphorylation of Phospholamban (PLB)
_______ stimulation increases inotropy
Little parasympathetic regulation of inotropy
Sympathetic
Phosphorylation increases Ca2+ sensitivity,
Increases inotropy by increasing SR Ca2+ release.
PKA phosphorylation of Ryanodine Receptor (RyR)
Phosphorylation slows inactivation, increases entry of trigger Ca2+
Increased Ca2+-induced Ca2+ release increases inotropy
PKA phosphorylation of L-type Ca2+ channel (DHPR)
decreases Ca2+ sensitivity of troponin C
allows faster dissociation of Ca2+ so faster filling = increased lusitropy (not inotropy)
PKA phosphorylation of Troponin I (TnI)
chronotropy
Chronotropic effects are those that change the heart rate.
Propranolol blocks β adrenergic receptors ___________
(sympathetic)