Receptors (MOAs) Flashcards
(40 cards)
What type of receptor is responsible for skeletal muscle contraction at the neuromuscular junction?
Nicotinic receptor (ionotropic), activated by acetylcholine.
What happens when acetylcholine binds to nicotinic receptors in skeletal muscle?
Depolarization occurs, activating dihydropyridine receptors which then open ryanodine receptors, releasing Ca²⁺.
What is the function of ryanodine receptors in skeletal muscle contraction?
They release calcium from the sarcoplasmic reticulum into the cytoplasm.
How does calcium lead to skeletal muscle contraction?
Calcium binds troponin C, shifts tropomyosin, exposes myosin-binding sites on actin, enabling contraction.
What role does ATP play in skeletal muscle contraction?
ATP binds to myosin, enabling the myosin head to pull actin for contraction.
Which neurotransmitter activates M3 muscarinic receptors?
Acetylcholine (ACh), released from parasympathetic postganglionic neurons.
What is the signal transduction pathway of M3 muscarinic receptors?
Activates Gq → PLC → PIP2 → IP3 + DAG → intracellular Ca²⁺ release and PKC activation.
What effect does IP3 have inside the cell?
It stimulates the release of Ca²⁺ from intracellular stores.
What is the effect of DAG in M3 receptor activation?
Activates protein kinase C (PKC), which contributes to smooth muscle contraction.
How does M3 receptor activation affect smooth muscle?
Leads to Ca²⁺-dependent activation of MLCK → contraction.
Where are β1-adrenergic receptors primarily found?
In the heart (SAN, AVN, myocardium) and kidney juxtaglomerular cells.
What intracellular pathway is activated by β1-adrenergic receptors?
Gs protein → adenylyl cyclase → cAMP → PKA activation.
What are the physiological effects of β1 receptor activation?
Increased heart rate, contractility, and renin release.
How does PKA increase heart contractility?
It phosphorylates Ca²⁺ channels, increasing calcium influx into cells.
Where are β2-adrenergic receptors found?
Bronchial and vascular smooth muscle.
What is the intracellular pathway of β2 receptor activation?
Gs protein → adenylyl cyclase → ↑ cAMP → PKA activation.
What does PKA do in β2-adrenergic signaling?
Inhibits MLCK, preventing smooth muscle contraction → relaxation.
What are the physiological effects of β2 receptor activation?
Bronchodilation, vasodilation, and smooth muscle relaxation.
Where are α1-adrenergic receptors located?
Vascular smooth muscle.
What signaling pathway do α1 receptors use?
Gq → PLC → IP3 + DAG → Ca²⁺ release and PKC activation.
What is the effect of α1 receptor activation?
Vasoconstriction and increased blood pressure.
Where are α2-adrenergic receptors located?
Presynaptic terminals.
What is the function of α2-adrenergic receptors?
Inhibit adenylyl cyclase → ↓ cAMP → ↓ neurotransmitter release (negative feedback).
Which G protein is associated with α2-adrenergic receptors?
Gi protein, which inhibits adenylyl cyclase.