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Ph 4 > Intro To CNS > Flashcards

Intro To CNS Flashcards

0
Q

Describe the small molecules neurotransmitters.

A

They are:

  • “classical” low-molecular weight neurotransmitter substances
  • there are many biochemical similarities including biosynthetic and degradation pathways.
  • all of these are amines and six derived from amino acids (ACh is the exception)
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1
Q

What are two major classes of neurotransmitters?

A

1) small molecules

2) peptides

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2
Q

What are the small molecule neurotransmitters?

A

1) acetylcholine (ACh)
2) dopamine (DA)
3) norepinephrine (NE)
4) epinephrine
5) serotonin (5HT)
6) glutamate
7) GABA

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3
Q

Describe peptide neurotransmitters.

A
  • These are also “small” molecules, these are typically larger than the ‘small molecules’.
  • There is an incredible diversity of peptide neurotransmitters in the brain.
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4
Q

What classes are included in the peptide neurotransmitters?

A

1) opioid-type peptides (like endorphins and enkephalins)
2) gut-brain peptides (like substance P)
3) hypothalamic-releasing hormones
4) the pituitary hormones

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5
Q

What is ACETYLCHOLINE?

A
  • ACh is an excitatory neurotransmitter used in the CNS and PNS.
  • In the PNS, ACh is used by motor neurons to trigger muscle contractions.
  • In the CNS, it maintains the electro-encephalographic (EEG) signals of the cortex and plays a role in memory by maintaining neuronal excitability.
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6
Q

How is Alzheimer’s disease related to ACh?

A

Alzheimer’s disease is related to the death of cholinergic (ACh-containing) neurons in the cortex.

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7
Q

What are the two types of ACh receptors?

A
  • 2 types of ACh receptors are : 1) muscarinic and 2) nicotinic.
  • Muscarinic ACh receptors are G-protein coupled receptors
  • nicotinic ACh receptors are ion channels
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8
Q

What is ACh made of?

A
  • ACh is made from acetyl-CoA and choline by the enzyme cholineacetyltransferase (ChAT).
  • acetyl-CoA is derived from the Krebs cycle in mitochondria
  • choline is only obtained from the diet and transported into neurons.
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9
Q

How is ACh eliminated?

A

ACh is eliminated by the enzyme acetylcholinesterase (AChE) that breaks down the neurotransmitter into choline and acetate.

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10
Q

ACh: What is an organophosphate-containing insecticides drug?

A

Malathion

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11
Q

ACh: What drug are nerve gases that are irreversible AChE inhibitors?

A

Sarin

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12
Q

What are used for Alzheimer’s symptoms?

A

Reversible AChE inhibitors

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13
Q

What is ACh receptor agonist?

A

Nicotine

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14
Q

What is a ACh receptor antagonist?

A

scopolamine

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15
Q

What are CATECHOLAMINES?

A

Catecholamines are a family of neurotransmitters that contain a “catechol” nucleus.

16
Q

What neurotransmitters are CATECHOLAMINES?

A

1) DOPAMINE
2) NOREPINEPHRINE
3) EPINEPHRINE

17
Q

What are the uses Dopamine?

A
  • Dopamine is involved in regulation of motor activity, motivation and reward, mood, sleep, learning, attention, etc.
  • Parkinson’s disease is related to the death of dopaminergic neurons in the substancia nigra (part of the subthalamus).
  • Reduced levels of dopamine may be related to attention deficit hyperactivity disorder (ADHD).
  • Too much dopamine may be related to schizophrenia.
18
Q

What are the uses of Norepinephrine?

A

Norepinephrine is involved in alertness, focus, positive feelings of reward.

19
Q

What are the uses of epinephrine ?

A

Epinephrine (also referred to as adrenalin) is involved in alertness and, together with NE, is part of the “fight-or-flight” stress response.

20
Q

How are catecholamines made?

A

-catecholamines are derived from the amino acid tyrosine by a series of enzymatic steps that convert tyrosine into dopamine, then into norepinephrine, then into epinephrine.

21
Q

How are catecholamines eliminated?

A

eliminated from the synaptic cleft by either

1) reuptake transporters or
2) by degradation enzymes (like monoamine oxidase [MAO] or catechol-O-metyltransferase [COMT]).

22
Q

What drugs disrupt reuptake transporters in catecholamines ?

A

1) cocaine

2) amphetamines

23
Q

What are used as antidepressants?

A

MAO inhibitors

24
Q

What are SEROTONIN?

A
  • Regulates aggression, emotional processing, mood, sleep, sexuality, appetite and metabolism.
  • Increases in levels of serotonin are related to obsessive-compulsive disorder and schizophrenia.
  • Decreases in levels of serotonin are related to depression.
25
Q

How is SEROTONIN made?

A
  • made from the amino acid tryptophan in two enzymatic steps.
  • Because tryptophan is an essential amino acid, it must be obtained from the diet and transported to neurons for use in serotonin biosynthesis
26
Q

How is serotonin eliminated?

A

It is eliminated by : 1) reuptake transporters or 2) by degradation enzymes (like monoamine oxidase [MAO

27
Q

What drugs disrupt serotonin reuptake transporters ?

A

cocaine and amphetamines

28
Q

What drug is a “selective serotonin reuptake inhibitor” (SSRI) that can be used instead of a non-selective MAO inhibitor?

A

Prozac (specific to serotonin)

29
Q

What are GLUTAMATE AND GABA?

A
  • Glutamate is the major excitatory neurotransmitter in the brain whereas GABA is the major inhibitory neurotransmitter in the brain.
  • Together, glutamate and GABA maintain the balance between excitation and inhibition in the brain.
  • Defects in either pathway can lead to epilepsy and seizures.
30
Q

How are Glutamates and GABA different from ACh, catecholamines and serotonin?

A

The neurotransmitters mentioned so far (ACh, catecholamines and serotonin) are made in a small subset of neurons by specific biochemical pathways.

In contrast, glutamate and GABA are made in most neurons and are also universal cellular constituents.

31
Q

How are glutamate and GABA made?

A
  • Glutamate is made from the amino acid glutamine by the enzyme glutaminase; it can also be derived as a byproduct of the Krebs cycle.
  • GABA is synthesized from glutamate by the enzyme glutamic acid decarboxylase (GAD).
32
Q

How are glutamate and GABA eliminated?

A

glutamate and GABA are eliminated from the synaptic cleft by either reuptake transporters or by degradation enzymes (GABA- transaminase) in neurons or glia.

33
Q

What drugs are agonists of the GABA receptor?

A

1) barbiturates
2) benzodiazepines
3) alcohol (ethanol)

34
Q

What are OPIOIDS?

A
  • Opioid type of peptide neurotransmitters are made of small chains of amino acids (polypeptides) derived from cleavage of larger precursor proteins made in the nucleus of appropriate neurons
  • neurotransmitters are involved in pain perception and reward mechanisms.
35
Q

What are endorphins and enkephalins?

A
  • Endorphins are chains of 16 to 30 amino acids of specific sequence.
  • Enkephalins have shorter chains (about 5 amino acids).
36
Q

What are natural opiates made from the opium poppy?

A

1) morphine

2) codeine

37
Q

What drugs are agonists of endogenous opioid receptors?

A

1) morphine (natural)
2) codeine (natural)
3) heroin (synthetic, man-made)
4) oxycodone (synthetic, man-made)

38
Q

How are they stopped/ eliminated?

A

Signals are terminated by specific peptidases.

Ph 4 (7 decks)

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