Adrenergic Receptor- Agonists and Antagonists Flashcards
Alpha-1 Receptor Organs
Vascular Smooth Muscle
Pupillary Dilator Muscle
Alpha-2 Receptor Organs
Adrenergic and cholinergic nerve terminals
Beta-1 Receptor Organs
Heart
Juxtaglomerular Cells
Beta-2 Receptor Organs
Respiratory Smooth Muscle
Uterine smooth muscle
Vascular smooth muscle
Somatic Motor nerve terminals
Dopamine 1 Receptors
Renal vessels
Sphlancinc Vessels
Alpha-1 signaling
Positively coupled to Phospholipase C by G-alpha-q to increase IP3 and DAG.
IP3 causes calcium channels to open and increase- activating calmodulin and MLCK for muscle contraction
Alpha-2 Signaling
Negatively coupled to adenylyl cyclase by G-alpha-i to inhibit PKA activation, cAMP and therefore calcium influx in order to reduce propagation and release of neurotransmitter in pre-synaptic neurons. Also in vascular smooth muscle- inactivated PKA= activated MLCK and therefore constriction.
Beta-1 Signaling
Positively coupled to adenylyl cyclase by G-alpha-s. Increasing cAMP and having positive chonotropic and ionotropic effects due to PKA activation and therefore high calcium.
SA Node
Beta-1 activated G-alpha-s. AC-cAMP-PKA causes increased calcium channel and IF to reduce threshold of activation and more rapid depolarization
Myocytes
Beta-1 activated G-alpha-s. AC-cAMP-PKA that increases L-type calcium channels, ryanodine receptor on SR and SERCA
Sympathetic nerve terminals
Negative feedback to alpha-2 G-alpha-i that inhibits AC, cAMP and PKA to decrease calcium propagation and therefore no NT release
Vascular smooth muscle
Alpha-1 coupled to G-alpha-q stimulates phospholipase C to increase PIP2 to IP3 and increase calcium for muscle contraction by MLCK
Direct Acting Adrenergic Agonists
A1- phenylephrine A2- Clonidine BNS- Isoproterenol B1- Dobutamine B2- Terbutaline, Albuterol
Indirect Acting Adrenergic Agonists
Releasing- amphetamine, methamphetamine, methylphenidate, ephedrine, pseudoephedrine, tyramine
alpha-1 affinities
Epinephrine >= Norepinephrine»_space;» isoproterenol
alpha-2 affinities
Epinephrine >= Norepinephrine»_space;» isoproterenol
beta-1 affinities
isoproterenol > epinephrine»_space;» norepinephrine
beta-2 affinities
isoproterenol > epinephrine = norepinephrine