Adrenergic Pharmacology of the ANS Flashcards
What transmitter is mostly released from postganglionic sympathetic neurons?
NE.
Which system relies mostly on DA?
Renal system
Transmitter of eccrine sweat glands?
ACh. Eccrine = thermoregulatory
A1 Receptors
Activate Gq, PLC, hydrolyze PIP2 to IP3 and DAG, PKC activation and release of intracellular Ca. Mediate contraction of smooth muscle. Are not in bronchioles and heart.
Where are A1 receptors absent from?
Bronchioles and Heart
What do all B receptors couple to?
Gs, causing relaxation of smooth muscle and increased contraction of cardiac muscle.
Which receptor type predominates in heart?
B1. B1 in atria and ventricles. B2 just in atria.
Which receptor type predominates in bronchioles and skeletal muscle vasculature?
B2, which dilates them.
Epinephrine
Non-selective adrenergic agonist. Activates A1 B1 and B2. Constricts most arterioles, but dilates skeletal vessels. BP may decrease. Direct effects on heart: increased heart rate and contractile force. Dilates bronchioles.
NE
Non-selective adrenergic agonist, but weak at B2. Large increase in BP, heart rate DECREASES. Large increase in BP because of activation of alpha receptors. Although B1 activated which should increase HR, baroreceptor response overwhelms it.
Isoproterenol
Non-selective B agonist, activates both B1 and B2. Dilates skeletal muscle arterioles, decreases systolic BP. Increased heart rate and contractile force, large increase in pulse pressure. Baroreceptor reflex in same direction as direct effects on heart (increased). Bronchioles dilated.
Phenylephrine
Alpha receptor agonist. Constricts vasculature, increases diastolic BP, decreases heart rate from baroreceptor reflex. No effect on airway.
Phentolamine
Alpha receptor antagonist. Dilates vasculature, decreases diastolic BP, increases heart rate from baroreceptor reflex. Often causes fainting. Given to people with pheochromocytoma (tumor of adrenal gland, who produce too much epi)
Propranolol
Nonselective B antagonist. Constricts vasculature, increase BP acutely (which decreases later due to other mechanisms, HR drops (direct and baroreflex), constricts airway.
Metoprolol
B1 Antagonist. Construct vasculature, increases BP, HR drops, no effect on airway (which are B2).