Norepinephrine: Alpha and Beta Receptors

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Questions and Answers

Alpha receptors are activated by which neurotransmitter?

  • Serotonin
  • Dopamine
  • Norepinephrine (correct)
  • GABA

Which second messenger is used by Alpha-1 receptors?

  • Adenylate cyclase (AC)
  • Guanylate cyclase (GC)
  • Tyrosine kinase (TK)
  • Phospholipase C (PLC) (correct)

What is the primary effect of activating Alpha-2 receptors?

  • Muscle contraction
  • Increased heart rate
  • Increased sodium influx
  • Decreased cAMP levels (correct)

Which ion channel is primarily affected by Alpha-2 receptor activation?

<p>Potassium (K⁺) (B)</p> Signup and view all the answers

What is the general effect of beta receptor activation?

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

All beta receptors increase the levels of which second messenger?

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

Which of the following is a primary effect of Beta-2 receptor activation?

<p>Smooth muscle relaxation (A)</p> Signup and view all the answers

Where are Beta-3 receptors primarily located?

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

What is the role of the norepinephrine transporter (NET)?

<p>Clearing norepinephrine from the synapse (C)</p> Signup and view all the answers

Which of the following drugs blocks the norepinephrine transporter (NET)?

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

Which enzyme is primarily responsible for the breakdown of norepinephrine?

<p>Monoamine Oxidase (MAO) (B)</p> Signup and view all the answers

What is the final breakdown product of norepinephrine?

<p>Vanillylmandelic acid (VMA) (A)</p> Signup and view all the answers

What type of drug is Moclobemide?

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

What is a common effect of drugs that inhibit NET?

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

Alpha-2 receptors act as what form of receptor?

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

Which of the following is a function of Beta-1 receptors?

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

What condition might be treated with a Beta-2 agonist like Salbutamol?

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

How does cocaine affect norepinephrine levels in the synapse?

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

What is one potential use of measuring VMA levels in urine?

<p>Assessing norepinephrine metabolism (B)</p> Signup and view all the answers

How does Moclobemide affect norepinephrine availability?

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

Alpha-1 receptor activation primarily leads to an influx of which ion?

<p>Calcium (Ca²⁺) (D)</p> Signup and view all the answers

Which type of receptors, when activated, generally cause excitation?

<p>All Beta receptors (B)</p> Signup and view all the answers

What is the effect of potassium efflux caused by Alpha-2 receptor activation?

<p>Decreased neuron excitability (D)</p> Signup and view all the answers

What does increased cAMP production generally lead to?

<p>Opening of sodium ion gates (C)</p> Signup and view all the answers

Which of these locations is most associated with Beta-2 receptors?

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

In which cellular component does Monoamine Oxidase (MAO) primarily function?

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

Which cellular process is promoted by NET?

<p>Reuptake of norepinephrine (B)</p> Signup and view all the answers

In the context of norepinephrine, what does 'metabotropic' mean?

<p>Working through second messengers (D)</p> Signup and view all the answers

What occurs when norepinephrine binds to Alpha-2 autoreceptors?

<p>Decreased norepinephrine release (B)</p> Signup and view all the answers

What is the action of drugs such as amphetamines on NET?

<p>Block NET, preventing norepinephrine reuptake (C)</p> Signup and view all the answers

Which of the following is an effect caused by a decrease in cAMP production?

<p>Inhibition of certain cellular functions (B)</p> Signup and view all the answers

Which receptor type is significant for regulating metabolism and fat breakdown?

<p>Beta-3 receptor (D)</p> Signup and view all the answers

What is the primary result of blocking NET?

<p>Increased levels of norepinephrine (A)</p> Signup and view all the answers

Which of the following is a potential therapeutic effect of MAO inhibitors?

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

What role does calcium influx play in neurons when Alpha-1 receptors are activated?

<p>Makes the neuron more excitable (C)</p> Signup and view all the answers

What effect does increased cAMP have on sodium ion (Na⁺) gates?

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

What process is dysregulated when there is too much norepinephrine in the synapse?

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

What condition may result from having too little norepinephrine?

<p>Low energy or depression (B)</p> Signup and view all the answers

What does Moclobemide act as for norepinephrine?

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

Which second messenger do Alpha-1 receptors use?

<p>Phospholipase C (PLC) (D)</p> Signup and view all the answers

What effect does increased cAMP production generally have?

<p>Opening sodium ion gates (B)</p> Signup and view all the answers

What is the term for the process where NET removes norepinephrine from the synapse?

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

What is the final breakdown product of norepinephrine metabolism?

<p>Vanillylmandelic acid (VMA) (C)</p> Signup and view all the answers

Flashcards

Alpha Receptors

Work through second messengers, activated by norepinephrine (NE), effects vary by subtype.

Alpha-1 Receptors

Use phospholipase C (PLC), leading to Ca²⁺ influx, increasing neuron excitability (EPSP).

Alpha-2 Receptors

Reduce cAMP, cause K⁺ efflux (IPSP), autoreceptors that regulate norepinephrine release.

Beta Receptors

Increase cAMP levels, leading to sodium ion influx and increased neuronal excitability.

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Beta-1 Receptors

Increase heart rate and neuronal activity. Important for alertness and arousal.

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Beta-2 Receptors

Cause smooth muscle relaxation (e.g., bronchodilation in lungs).

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Beta-3 Receptors

Help regulate metabolism and fat breakdown.

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Norepinephrine Transporter (NET)

Clears norepinephrine from the synapse, stopping its action; maintains optimal NE levels.

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Cocaine & Amphetamines (effect on NET)

Block NET, keeping norepinephrine in the synapse longer, leading to increased stimulation.

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Monoamine Oxidase (MAO)

Breaks down norepinephrine after reuptake in the neuron.

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Vanillylmandelic acid (VMA)

Final breakdown product of norepinephrine, measured to assess NE metabolism.

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MAO Inhibitors (MAOIs)

Prevents NE breakdown, increasing available NE, treating depression and low energy.

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Study Notes

  • Norepinephrine (NE) activates alpha receptors, which are metabotropic receptors that operate through second messengers rather than directly opening ion channels.

Alpha-1 Receptors

  • These receptors are excitatory and use phospholipase C (PLC) as a second messenger.
  • Calcium influx occurs, making the neuron more excitable, resulting in an excitatory postsynaptic potential (EPSP).
  • Decreases cAMP (cyclic adenosine monophosphate) production.

Alpha-2 Receptors

  • Alpha-2 receptors are inhibitory and also act as autoreceptors.
  • cAMP levels are reduced, thus inhibiting certain cellular functions.
  • Causes potassium efflux and leads to an inhibitory postsynaptic potential (IPSP), which makes the neuron less likely to fire.
  • They regulate norepinephrine release by sensing NE levels in the synapse and reducing further release, if needed.

Beta Receptors

  • Increases cAMP levels.
  • Higher cAMP levels lead to the opening of sodium ion gates, making neurons more excitable.
  • Beta receptor activation generally leads to excitation.

Beta-1 Receptors

  • Primarily located in the heart and brain
  • Increases heart rate and neuronal activity.
  • Important for alertness and arousal.

Beta-2 Receptors

  • Found mostly in the lungs and muscles
  • Causes smooth muscle relaxation, such as bronchodilation in the lungs.
  • Used as treatments for asthma, such as Salbutamol.

Beta-3 Receptors

  • Located in fat cells
  • Regulate metabolism and fat breakdown.

Norepinephrine Transporter (NET)

  • Responsible for reuptake.
  • It clears norepinephrine from the synapse to stop its action.
  • Insufficient norepinephrine can lead to low energy or depression, whereas too much norepinephrine can cause overstimulation.
  • Cocaine and amphetamines block NET, which keeps norepinephrine in the synapse longer and leads to increased stimulation.

Enzymatic Degradation of Norepinephrine

  • Monoamine Oxidase (MAO) mainly breaks down NE after it is taken back into the neuron.
  • Vanillylmandelic acid (VMA) is the final breakdown product of norepinephrine.
  • VMA levels in urine are measured to assess norepinephrine metabolism and diagnose diseases like pheochromocytoma.

MAO Inhibitors (MAOIs)

  • Moclobemide, which is an MAO inhibitor, prevents NE breakdown, thus keeping more of it available.
  • Acts as an agonist, or enhancer, for norepinephrine, which helps treat depression and low energy.

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