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PSYCH 478 > Serotonin > Flashcards

Serotonin Flashcards

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1
Q

____________ are a group of NTs/hormones that share a common single AMINE functional group.

A

monoamines

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2
Q

90% of the 5HT in your body is found in the ______.

A

gut

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3
Q

5-HT is a major NT in the _________________ and is released by ______________ cells.

A

enteric nervous system; enterochromaffin

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4
Q

5HT stimulates ________ and secretion into the intestines.

A

peristalsis

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5
Q

5HT is massively released in response to chemical, physical, and pathological stimuli and can activate __________ __________ to signal the brain in generation of nausea & act at the ________ ___________ (chemoreceptor trigger zone).

A

vagal afferents; area postrema

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6
Q

What is the area postrema?

A

chemoreceptor trigger zone

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7
Q

________ _______________ is transported into the brain where it is converted to 5HT by _______ _____________.

A

dietary L-tryptophan; tryptophan hydroxylase

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8
Q

What is the rate limiting enzyme in the production of 5HT?

A

tryptophan hydroxylase

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9
Q

5HT is deaminated by ____________ ___________ to _______________ ____________ in the cytoplasm of _____________ neurons.

A

monoamine oxidase; 5-hydroxyindoleacetic acid; serotonergic

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10
Q

In contrast to the catecholamines, 5HT breakdown occurs only through ________.

A

MAO

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11
Q

Describe the enzymes and pathway of 5HT synthesis and catabolism

A

L-tryptophan –tryptophan hydroxylase–> 5-HTP –decarboxylase–> 5HT –MAO–> 5-HIAA

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12
Q

REVIEW slide 5 diagram

A

slide 5

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13
Q

_________________ (__________) is used in animals to rapidly deplete 5HT.

A

para-chlorophenylalanine (PCPA)

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14
Q

TRUE or FALSE: PCPA is a reversible antagonist of tryptophan hydroxylase.

A

FALSE: irreversible inhibitor

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15
Q

PCPA is an irreversible inhibitor of ________________.

A

tryptophan hydroxylase

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16
Q

1-2 doses of PCPA depletes 5HT by up to _____% for up to ___ weeks.

A

90; 2

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17
Q

______________ also depletes 5HT by inhibiting VMAT.

A

reserpine

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18
Q

Tryptophan can be depleted in humans by administering an amino acid mix devoid of ____________.

A

tryptophan

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19
Q

How does an amino acid mix devoid of tryptophan deplete tryptophan in humans?

A
  • boost of AAs triggers protein synthesis in liver, depleting previous supply of tryptophan
  • neutral AAs compete for BBB transporters
20
Q

Which substances can be used for tryptophan/5HT depletion? What is the mechanism?

A
  • PCPA - irreversible inhibitor of tryptophan hydroxylase
  • reserpine - inhibit VMAT
  • AA mix w/o tryptophan - protein synthesis depletes previous supply of tryptophan
21
Q

TRUE or FALSE: tryptophan-containing mixture will lead to a more sad mood, in comparison to a tryptophan-free mixture

A

FALSE: no tryptophan = more sad

22
Q

review sllide 8 diagram

A

slide 8

23
Q

What are some 5-HT releasers? What are they typically used for?

A
  • fenfluramine - weight loss in obesity
  • para-chloroamphetamine - experimental amphetamine analogue
  • 3,4-methylenendioxymethamphetamine (MDMA) - psychoactive recreational drug (Ecstasy)
24
Q

TRUE or FALSE: fenfluramine is a 5HT depleter

A

FALSE: 5HT releaser

25
Q

Which 2 NTs are directly opposed in regulating appetite?

A

dopamine and 5HT

26
Q

How does dopamine regulate appetite?

A
  • stimulate appetite
  • released in response to food stimuli (smell)
27
Q

How does 5HT regulate appetite?

A
  • decrease appetite
  • released in response to eating
  • inhibits dopamine release
28
Q

___________________ suppresses appetite through effects on catecholamines (psychostimulant like amphetamine)

A

phentermine

29
Q

__________ came into use in the 1990s as an off-label prescription for obesity.

A

Fen-Phen (fenfluramine-phentermine)

30
Q

Why is phentermine used with fenfluramine in treating obesity?

A

co-treatmen avoided DROWSINESS and ADVERSE MOOD effects associated with fenfluramine

31
Q

review graph on slide 11

A

slide 11

32
Q

TRUE or FALSE: Fen-Phen is FDA approved for weight loss

A

FALSE: never FDA approved

33
Q

What severe adverse consequences are linked with long-term Fen-Phen use?

A
  • heart valve abnormalities
  • primary pulmonary hypertension - increased BP between heart and lungs (often fatal)
34
Q

Both fenfluramine and dexfenfluramine removed from clinical used in late __________.

A

1997

35
Q

What class of transporters is responsible for inactivation of 5HT signalling by reuptake?

A

5HT transporters (SERT)

36
Q

SERT is similar to _____ and ________.

A

DAT; NAT

37
Q

TRUE or FALSE: many drugs jave effects at all 3 transporters (SERT, DAT, NET)

A

TRUE

38
Q

SERT also found in __________, ___________, and _____________.

A

lungs, placenta, platelets

39
Q

SERT pumps systemic 5HT into ___________.

A

platelets

40
Q

TRUE or FALSE: SERT functions in clotting cascades as a vasodilator.

A

FALSE: vasoconstrictor

41
Q

TRUE or FALSE: SERT is a popular drug target

A

TRUE

42
Q

Which drug classes target SERT? Which ones are selective/non-selective?

A
  • TCA antidepressants (non-selective for SERT, NET)
  • SSRI antidepressants (selective for SERT)
  • SNRI antidepressants (non-selective for SERT, NET)
  • SNDRI antidepressants (SERT~NET>DAT)
  • psychoactive drugs (non-selective for SERT, NET, DAT)
43
Q

What class of drugs does imipramine belong to?

A

TCA antidepressants

44
Q

What class of drugs does fluoxetine belong to?

A

SSRI antidepressants

45
Q

What class of drugs does venlafaxine belong to?

A

SNRI antidepressants

46
Q

What class of drugs do cocaine, amphetamines, MDMA belong to?

A

psychoactive drugs

PSYCH 478 (28 decks)

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