Catecholamines Flashcards

1
Q

The enzyme required for Tyrosine—–>DOPA??.

A

Tyrosine hydroxylase.

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2
Q

The enzyme required to convert DOPA—->Dopamine??.

A

Aromatic amino acid decarboxylase(AADC).

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3
Q

The enzyme to convert dopamine—–>Norepinephrine??

A

Dopamine B-hydroxylase.

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4
Q

Packaging of catecholamines?

A
  • Achieved via Vesicular monoamine transporter(VMAT).
  • released via exocytosis.
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5
Q

Functions of;

  • Amphetamines?
  • Reserpine?
A

Amphetamines:

  • increase cell firing.

Reserpine:

  • Block DA uptake in VMAT2,
    • results in depression and sedation.
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6
Q
  • The function of Autoreceptor D2 autoreceptors?

How does it achieve this function?

what type of autoreceptor are they?

A

Overall function: inhibits catecholamine release.

  • Enhances opening of K+ channels, hyperpolarisation.

therefore:

  • reduces AP and Ca2+ influx.
  • Somatodendritic autoreceptor.
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7
Q

The function of transporter proteins?

A
  • Allow the reuptake of NE and DA.
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8
Q

Role of Tricyclic antidepressants?

A
  • Inhibit reuptake of both NE and Serotonin.
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9
Q

Neurophysiology of cocaine?

A
  • inhibits the reuptake of all mono-amine transmitters:

DA,5-HT, and NE.

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10
Q

Function of Roboxetine( edronax)?

Function of Atomexetine(Strattera)?

A
  • Roboxetine : antidepressant, blocking NE transporters(reuptake)
  • Atomoxetine (Strattera):
    • Used for ADHD to block NE transporters.
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11
Q

The difference in function between Catechol-O-methyltransferase(COMT) AND Monoamine oxidase(MAO)??

A

COMT: degrades and breakdown dopamine.

MAO: degrade and breakdown of NE.

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12
Q

Metabolites of DA and NE??

A
  • DA: Homovanillic acid.
  • NE: CNS: MHPG and PNS: VMA.
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13
Q

How can levels of catecholamine levels be measured?

A
  • Measuring the levels of metabolites within urine, e.g. Homovanillic acid for DA.
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14
Q

Function of Phenelzine(Nardil) and Tranylcypromine(Parnate)?

A
  • Are MAO inhibitors, which inhibit metabolism and breakdown of NE.
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15
Q

Function of Entacapone(Comtan) and Tolcapone(Tasmar)?

A
  • inhibition of COMT, inhibits breakdown of DA.

Enhances the functioning of L-DOPA for PD.

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16
Q

What cell group classification system correspond to NE and DA?

A
  • NE= A1-A7.
  • DA= A8-16.
17
Q

Describe the Nigrostriatal pathway:

  • from where—where?
  • Cell groups?
A
  • Substantia nigra———-

–>Striatum.

or

–>caudate putamen.

A9 CELL GROUP.

18
Q

Describe the mesolimbic dopamine pathway;

Cell groups and projections?

A
  • A10 cell group.
  • VTA——-
    • –> limbic system( Nucleus accumbens and Olfactory tubercules).
19
Q

Describe the mesocortical dopamine pathway.

  • Cell group and projections?.
A
  • A10 cell group.
  • VTA——–>
  • –>prefrontal cortex.
20
Q

State the significance of the nigrostriatal pathway to PD models?

toxins used as a model for PD?

A
  • Fascilitates voluntary movement.
  • PD involves the loss of DA neurons from the SN, which leads to denervation of the striatum.

Neurotoxins:

  • 6-OHDA and MPTP: damage the nigrostriatal pathway.
21
Q

State the type of receptor DA receptors are.

  • Briefly state the mechanism in activation of these receptors?
  • State the receptors within D1-like receptors and D2-like receptors.
A

Metabotropic receptors:

  • interacting with G-proteins and function as secondary messengers.

D1-like receptors: D1 and D5.

D2-like receptors: D2-D4.

22
Q

Activation of:

D1 receptors and D2 receptors?

A

D1 receptors:

  • stimulates adenylyl cyclase and synthesis of cAMP.

D2 receptors:

  • inhibits adenylyl cyclase and synthesis of cAMP.
  • Opening of K+ channels, as activation of G-protein enhances K+ opening.
23
Q

Receptor-selective drugs: AGONISTS.

  • Function of:
    • SKF 38393.
    • Quinpirole.
    • Apomorphine.
A

SKF 38393:

  • Is an agonist for D1 receptors.

Quinpirole:

  • activates D2 and D3 receptors.

Apomorphine:

  • agonist stimulating D1 and D2
24
Q

Receptor selective ANTAGONISTS.

Uses and function of Haliporidol and SCH 23390.

A

Function:

  • Suppressor of locomotor and exploratory movement.

Haloperidol; D2 receptor blockers.

SCH 23390: D1 receptor blockers.

25
Q

Mice knockout:

D1 knockout?

D2 knockout?

Both knockout?

D4 knockout?

A
  • D1 receptor knockout: deficits in cognitive tasks.
  • D2 receptor knockout: impairment in spontaneous movement, coordination, and posture.

Both: leading to fatality in the 2nd and 3rd week of life.

  • D4 receptor knockout: hypersensitive to cocaine and methamphetamines.
26
Q

Quick overview of the drugs.

A
27
Q

Describe the Locus Coerulus(LC) in pons:

  • Group of cells?
  • Projections?
A
  • A6 cell group.
  • Projections from pons to——-

—> all areas of the forebrain.

—> cerebellum and spinal cord.

28
Q

Describe the adrenoreceptors?

  • type of receptor?
  • 2 groups.
A
  • Metabotropic receptors:

alpha and beta.

a2: reduces cAMP synthesis.
a1: operates via phosphoinositide second messenger system.

B1 and B2:

  • stimulate adenylyl cyclase and enhance cAMP.(like D1 receptors).