MMT: Pharmacology of Autonomic Drugs Flashcards
try not to cry
what are the two main classes of receptors?
cholinergic and adrenergic
what are the two subdivisions of cholinergic receptors? what are their methods of action?
Muscarinic: GPCRs
Nicotinic: ion channels that are permeable to cations, particularly Na.
Which muscarinic receptors are associated with Gq? What is the significance of this?
M1, M3, M5. Since they’re associated with Gq, they all stimulate the release of calcium and thus the contraction of smooth muscle
Which muscarinic receptors are associated with Gi? What is the significance of this?
M2 and M4. They’re associated with lowering cAMP and increasing potassium efflux, which leads to hyperpolarization. They’re also associated with lowered PKA, which decreases Ca channel activity. This slows AP conduction
what are the subdivisions of adrenergic receptors?
alpha and beta
what is the method of action for adrenergic receptors?
GPCR
Describe alpha1-adrenergic receptors: general effect, what they’re coupled to, their downstream effect, and what they stimulate
They’re typically excitatory and regulate the SNS. They’re coupled to Gq and increase calcium release via IP3. they stimulate the constriction of smooth muscle.
Describe alpha2-adrenergic receptors
They’re typically inhibitory and reduce sympathetic outflow. They’re coupled to Gi. They’re present on presynaptic nerve terminals and prevent norepinephrine release via a negative-feedback mechanisms. If there is too much NE in the synaptic cleft, it acts of alpha2 receptors and prevent further NE release
Describe beta1-adrenergic receptors: general effect, their downstream effector, what they stimulate
They’re excitatory and regulate the SNS. They are coupled to Gs, and stimulate cAMP and contraction of heart muscle
describe beta2-adrenergic receptors: general effect, what they’re coupled to, their downstream effect, and what they stimulate
They’re inhibitory and regulate the SNS. they are coupled to Gs, and stimulate cAMP and relaxation of smooth muscle.
Describe how increased cAMP impacts cardiac and smooth muscle
Increases cardiac muscle contraction, but relaxes smooth muscle
SA node: sympathetic receptor and nervous system response vs parasympathetic receptor and nervous system response
Sympathetic b1 receptor, increased heart rate
Parasympathetic m2 receptor, decreased heart rate
AV node: sympathetic receptor and nervous system response vs parasympathetic receptor and nervous system response
Sympathetic b1 receptor increases conduction, parasympathetic m2 receptor decreases conduction
Atria: sympathetic receptor and nervous system response vs parasympathetic receptor and nervous system response
Sympathetic b1 receptor increases contractility, parasympathetic m2 receptor decreases contractility
ventricles: sympathetic receptor and nervous system response vs parasympathetic receptor and nervous system response
sympathetic b1 receptor increases contractility, and parasympathetic m receptor decreases contractility; actions of PSNS are almost negligible.