Adrenergic receptors Flashcards
Alpha-1 receptors
Are on vascular smooth muscle, mediated vasoconstriction
Gq coupled, PLC, IP3 and DAG, Ca++
NE > E
Alpha-2 receptors
The Presynaptic Adrenergic autoreceptor
Gi/Go coupled, hyperpolarizing presynaptic channel, opens K+ channels and inhibits Ca++ channels
Beta-1 receptors
Cardiac myocyte adrenergic receptors
Gs coupled
Inotropic, via PKA activation, and its phosphorylation of:
L-type VDCCs, increases their activity
Phospholamban, PKA inhibits phospholamban, disinhibiting a Sarcoplasmic Ca++ pump, and thereby increasing the sarcoplasmic Ca++ concentration, causing greater Ca++ release on activation and more powerful contraction.
E==NE
Mechanism of cardiac glycosides action
INHIBITS the Na/K pump,
Increases intracellular Na+
Decreases activity of the Na+/Ca++ exchanger, causing less Ca++ to be pumped out of the cell.
Increasing Ca++ intracellularly as well.
Beta-2 receptors
On very FEW, specific vascular smooth muscle populations
Coronary vessels,
some skeletal vessels
Gs coupled,
elevates cAMP, PKA activates mysoin phosphorylase, relaxation
is the ONLY adrenergic receptor that is more sensitive to epinephrine
Epinephrine» NE
Beta-3 receptors
on adipose
Gs
Ne>E