Adrenergic Receptor Types and Effects

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Questions and Answers

Which of the following signaling pathways is activated by the α1 receptor?

  • Activation of phospholipase C (PLC) leading to increased DAG and IP3. (correct)
  • Activation of adenylyl cyclase leading to increased cAMP.
  • Inhibition of adenylyl cyclase leading to decreased cAMP.
  • Direct activation of Rho kinase.

What is the primary effect of stimulating β2 receptors in bronchial smooth muscle?

  • Bronchodilation (correct)
  • Bronchoconstriction
  • Increased mucus production
  • Decreased pulmonary blood flow

Which of the following is a downstream effect of M2 receptor activation in the heart?

  • Increased calcium influx
  • Decreased cAMP and inhibition of MLCK (correct)
  • Increased heart rate and contractility
  • Activation of adenylyl cyclase

Which G-protein class is associated with the α2 receptor?

<p>Gi (A)</p> Signup and view all the answers

What is the effect of α1 receptor activation on vascular smooth muscle?

<p>Vasoconstriction (C)</p> Signup and view all the answers

Which second messenger is directly increased as a result of β1 receptor stimulation in the heart?

<p>cAMP (A)</p> Signup and view all the answers

What is the result of activating Rho kinase in smooth muscle?

<p>Inhibition of MLCP, promoting contraction. (D)</p> Signup and view all the answers

Which receptor, when stimulated, leads to a decrease in sympathetic outflow from presynaptic nerve terminals?

<p>α2 receptor (C)</p> Signup and view all the answers

What is the direct effect of stimulating the M3 receptor on bronchial smooth muscle?

<p>Bronchoconstriction (C)</p> Signup and view all the answers

Which of the following receptors, when activated, primarily increases heart rate and contractility?

<p>β1 Receptor (C)</p> Signup and view all the answers

Activation of which receptor leads to increased renin release from the kidney?

<p>β1 (D)</p> Signup and view all the answers

Which second messenger system is utilized by the M3 receptor to exert its effects?

<p>Phospholipase C / IP3 and DAG (B)</p> Signup and view all the answers

What effect does the activation of the α2 receptor have on cAMP levels inside the cell?

<p>Decreases cAMP levels. (B)</p> Signup and view all the answers

In smooth muscle, increased intracellular calcium, resulting from IP3 stimulation, directly leads to:

<p>Activation of the Myosin Light Chain Kinase (MLCK) (A)</p> Signup and view all the answers

Which neurotransmitter primarily activates the M2 receptor?

<p>Acetylcholine (B)</p> Signup and view all the answers

Which of these events is a direct consequence of activating the Gq protein-coupled receptor?

<p>Activation of phospholipase C (A)</p> Signup and view all the answers

Based on the information, what effect would an agonist of the β2 receptor have on blood vessels in skeletal muscle?

<p>Vasodilation (A)</p> Signup and view all the answers

Which intracellular change would you expect to see after administering a drug that selectively activates M2 receptors?

<p>Decreased cAMP production (C)</p> Signup and view all the answers

How does activation of the α1 receptor lead to smooth muscle contraction?

<p>By increasing intracellular calcium through the IP3 pathway, which activates myosin light chain kinase. (D)</p> Signup and view all the answers

Which statement accurately describes the role of Myosin Light Chain Phosphatase (MLCP)?

<p>It dephosphorylates myosin light chains, leading to muscle relaxation. (B)</p> Signup and view all the answers

Flashcards

α1 Receptor

Receptor: α1; Neurotransmitter: NE; Tissue: VSM; G-protein class: q; Second messenger: Activates PLC, converts PIP2 to DAG + IP3

α2 Receptor

Receptor: α2; Neurotransmitter: NE; Tissue: Presynaptic nerve terminal; G-protein class: i; Second messenger: Inhibits adenylyl cyclase, decreases cAMP

β1 Receptor

Receptor: β1; Neurotransmitter: NE/Epi; Tissue: Heart, Kidney; G-protein class: s; Second messenger: Activates adenylyl cyclase, converts ATP to cAMP

β2 Receptor

Receptor: β2; Neurotransmitter: Epi; Tissue: VSM, bronchial smooth muscle; G-protein class: s; Second messenger: Activates adenylyl cyclase, converts ATP to cAMP

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M2 Receptor

Receptor: M2; Neurotransmitter: Ach; Tissue: Heart; G-protein class: i; Second messenger: Inhibits adenylyl cyclase, decreases cAMP

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M3 Receptor

Receptor: M3; Neurotransmitter: Ach; Tissue: Bronchial smooth muscle, endothelial cells; G-protein class: q; Second messenger: Activates PLC, converts PIP2 to DAG + IP3

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How Alpha-2 affects cAMP?

Inhibits adenylyl cyclase, leads to decreased cAMP, resulting in decreased sympathetic (adrenergic) outflow.

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How Alpha-1 affects PLC?

Activates PLC, which converts PIP2 into DAG and IP3, leading to increased VSM contraction and vasoconstriction.

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Beta-1's Second Messenger

Stimulates adenylyl cyclase, converting ATP to cAMP; this increases heart rate, contractility, and renin release.

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Beta-2's Effect on Adenylyl Cyclase

Activates adenylyl cyclase to increase cAMP leading to vasodilation and bronchodilation.

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M2's Effect on cAMP

Inhibits adenylyl cyclase, leading to a decrease in cAMP levels, reducing heart rate and contractility.

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M3's Second Messenger Pathway

Activates PLC, converting PIP2 to DAG and IP3. This results in bronchoconstriction and vasodilation.

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Study Notes

  • This table summarizes receptor activation/inhibition; consult topic notes for comprehensive details.

Receptor Types and Effects

α1 Receptor

  • Responds to Norepinephrine (NE)
  • Found in Vascular Smooth Muscle (VSM) and visceral smooth muscle.
  • G-protein class is q.
  • Activates PLC, converting PIP2 into DAG + IP3, leading to VSM contraction and vasoconstriction.
  • DAG stimulates PKC.
  • IP3 increases Ca release, forms Ca/Calmodulin complex, stimulates MLCK, leading to Myosin-P+actin contraction.
  • Activates Rho kinase, which inhibits MLCP.
  • Results in muscle contraction.

α2 Receptor

  • Responds to NE.
  • Located in presynaptic nerve terminals.
  • G-protein class is i.
  • Inhibits adenylyl cyclase, decreasing ATP to cAMP conversion, leading to reduced cAMP stimulation of PKA and decreased Ca.
  • Causes a decrease in sympathetic (adrenergic) outflow.

β1 Receptor

  • Responds to NE/Epi.
  • Found in the heart and kidney.
  • G-protein class is s.
  • Activates adenylyl cyclase, converting ATP to cAMP.
  • Increases heart rate (HR), contractility, and renin release.
  • cAMP stimulates PKA, increasing Ca release.

β2 Receptor

  • Responds to Epi.
  • Located in VSM and bronchial smooth muscle.
  • G-protein class is s.
  • Activates adenylyl cyclase, converting ATP to cAMP, resulting in vasodilation and bronchodilation.
  • cAMP stimulates PKA, which then increases Ca release.

M2 Receptor

  • Responds to Acetylcholine (Ach).
  • Found in the heart.
  • G-protein class is i.
  • Inhibits adenylyl cyclase, decreasing ATP to cAMP conversion.
  • Decreases HR and contractility.
  • Decreased cAMP stimulation of PKA leads to reduced Ca influx/release.

M3 Receptor

  • Responds to Ach.
  • Located in bronchial smooth muscle and endothelial cells.
  • G-protein class is q.
  • PLC converts PIP2 into DAG + IP3, leading to bronchodilation and vasodilation.
  • DAG stimulates PKC.
  • IP3 stimulates Ca release.

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