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Pharmacology FINAL > lecture 7 part 2 > Flashcards

lecture 7 part 2 Flashcards

1
Q

what does NPY stand for

A

neuropeptide Y

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2
Q

what is the primary function of neuropeptide Y (NPY)

A

causes long lasting vasoconstriction

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3
Q

what does NO stand for

A

nitric oxide

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4
Q

true or false

NO is not a neurotransmitter

A

false - it is

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5
Q

what does CCK stand for

A

cholecystokinin (neurotransmitter)

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6
Q

what is the role of cholecysokinin (CCK)

A

may act as a co-neurotransmitter in some excitatory neuromuscular ENS neurond

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7
Q

enkephalin is related to what?

A

opioid peptides

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8
Q

explain what enkephalin and opioid related peptides do

A

inhibit acetylcholine release and inhibit peristalsis.
may stimulate secretion

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9
Q

galanin may play a role in what?

A

appetite-satiety mechanisms

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10
Q

what does GABA stand for

A

gamma-amino butyric acid

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11
Q

explain what GABA does

A

has relaxant effects on the gut

probably not a major neurotransmitter in the ENS

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12
Q

what does GRP stand for

A

gastrin releasing peptide

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13
Q

explain what GRP (gastrin releasing peptide) does

A

an extremely potent excitatory neurotransmitter to GASTRIC CELLS (stomach)

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14
Q

true or false

the metabolic rate increasing is part of a sympathetic response

A

true

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15
Q

a sympathetic response will cause _______ digestive and urinary functions

A

decreased

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15
Q
A
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16
Q

true or false

a sympathetic response will cause an increase in blood pressure

A

true

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17
Q

true or false

a sympathetic response will cause a deactivation of energy reserves

A

FALSE - activation

this is why most ppl lose weight when stressed

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18
Q

true or false

sweat glands are activated in the sympathetic response

A

true

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19
Q

parasympathetic division causes _____ metabolic rate

A

decreased

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20
Q

true or false

the parasympathetic division causes the activation of sweat glands

A

false - activation of all other glands like salivary and digestive

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21
Q

most autonomic nervous system regulations use what kind of feedback?
how does this relate to drugs

A

NEGATIVE FEEDBACK

negative feedback is important in the responses of the ANS to autonomic drugs

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22
Q

name the autonomic receptors

A

cholinergic and adrenergic

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23
Q

further classify the autonomic receptors

A

cholinergic - nicotinic and muscarinic

adrenergic – alpha adrenergic (alpha1 and alpha2) and beta adrenergic (beta 1,2,3)

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24
Q

what is the result of ligand binding to M1

A

formation of IP3 and DAG and increased intracellular calcium (works thru Gq!)

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25
Q

what is the result of ligand binding to M2

A

the opening of potassium channels and inhibition of adenylyl cyclase
(decreased heart rate)

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26
Q

what is the result of ligand binding to M3

A

like M1 - formation of IP3 and DAG and increased intracellular calcium

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27
Q

what is the result of ligand binding to M4

A

like M2 - opening of potassium channels and inhibition of adenylyl cyclase

(decreased heart rate)

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28
Q

what is the result of ligand binding to M5

A

like M1 - formation of IP3 and DAG and increased intracellular calcium

29
Q

what are the typical locations of M1

A

CNS neurons

sympathetic postganglionic neurons

some presynaptic sites

30
Q

what are the typical locations of M2

A

myocardium and smooth muscle

31
Q

what are the primary locations of M3

A

exocrine glands

32
Q

what are the primary locations of M4

A

CNS neurons

33
Q

what are the primary locations of M5

A

vascular endothelium

34
Q

name the 2 nicotinic receptors

A

NN and NM

35
Q

what are the results of ligand binding to NN? what about ligand binding to NM?

A

both result in the opening of Na+ and K+ channels and DEPOLARIZATION

36
Q

further classify the adrenoceptors

A

alpha 1 and alpha 2

beta 1,2,3

36
Q

explain the result of ligand binding for beta1, beta2, and beta3 receptors

A

beta1 - contraction. stimulation of adenylyl cyclase and increased cAMP. found in heart and blood vessels

beta2 - relaxation. stimulation of adenylyl cyclase and increased cAMP. stimulates cardiac G under some conditions. found in smooth and cardiac muscle

beta3 - stimulation of adenylyl cyclase and increased cAMP. breaks down fats

37
Q

explain what alpha 1 and alpha 2 receptors do

A

alpha 1 contracts through formation of IP3 and increased intracellular calcium

alpha 2 relaxes through inhibiting adenylyl cyclase and decreases cAMP

38
Q

explain the typical locations of alpha 1 and alpha 2 receptors

A

alpha 1 - at postsynaptic effector cells especially smooth muscle

alpha 2 is at presynaptic adrenergic nerve terminals, platelets, lipocytes, and smooth muscle

39
Q

for someone with hypertension, what kind of beta blocker is needed?

A

a SELECTIVE beta1 blocker.
if it is effective on beta1 and beta2, the person wouldnt be able to breathe

40
Q

in general, what is the typical location of the dopamine receptors?

A

the brain

41
Q

name all of the dopamine receptors and the result of ligand binding

A

D1, D2, D3, D4

D1 - stimulation of adenylyl cyclase and increased cAMP

D2 - inhibition of adenylyl cyclase and increased potassium conductance

D3, D4 - inhibition of adenylyl cyclase

42
Q

name the 4 steps of acetylcholine transmission

A

synthesis
storage
release
action and termination

43
Q

what is the name of the enzyme that breaks down acetylcholine?
what is it broken into?

A

acetylcholine esterase breaks down acetylcholine into choline and acetate

choline can be recycled and acetate is released out

44
Q

explain how acetylcholine is synthesized and released

A

sodium and choline pass through the choline transporter on the membrane.

acCoA is from the mitochondria (from inside of the cell)

AcCoA and choline are joined toghether by ChAT (choline acetyltransferase)

newly formed acetylcholine is then transported into a vesicle through VAT (vesicular acetylcholine transporter)

acetylcholine is released from the vesicle when calcium enters the cytoplasm and through VAMPS (vesicle associated membrane proteins) exocytised with ATP and P

45
Q

what blocks the synthesis of acetylcholine and how?
what drugs mimic this?

A

hemicholiniums

will not allow the transport of choline across the membrane.

antipsychotic meds mimic this

46
Q

once acetylcholine has been synthesized, what happens

A

the acetycholine (now in the cytoplasm) needs to be stored in a vesicle

this is done through VAT (vesicular acetylcholine transporter)

47
Q

what blocks acetylcholine from going into the vesicle

A

vesamicol.

blocks VAT and thus no vesicle

48
Q

once acetylcholine is in the vesicle, what happens?

A

exocytosis out of the cell, and acetylcholine binds on its cholinergic receptor,

exocytosis occurs via VAMPs (vesicle associated membrane proteins) and the influx of calcium

49
Q

what blocks the exocytosis of acetylcholine?

A

botulinum toxin

50
Q

where is acetylCoA synthesized

A

in the mitochondria

51
Q

where are mitochondria present in large numbers?

A

in the nerve ending

52
Q

true or false

acetylcholine is synthesized in the cytoplasm

A

true

53
Q

what enzyme synthesizes acetylcholine

A

choline acetyltransferase (ChAT)

54
Q

what is VAT driven by?
what does VAT do?

A

VAT (vesicle associated transporter) transports the newly synthesized acetylcholine from the cytoplasm and into a vesicle.
it is driven by the efflux of protons

55
Q

VAT can be blocked by…

A

vesamicol

56
Q

most of the vesicular acetylcholine is bound to what?

A

VPG – negatively charged vesicular proteoglycan

57
Q

where are vesicles concentrated and by what?

A

on the inner surface of the nerve terminal by SNARE proteins on the vesicle and on the inside of the terminal cell membrane

58
Q

the release of acetylcholine from the vesicle is dependent on what

A

extracellular calcium

occurs when an action potential reaches the terminal and triggers sufficient influx of calcium ions

59
Q

what inhibits the reuptake of norepinephrine

A

cocaine and tricyclic antidepressants.

NE will thus stay in the synaptic cleft longer

60
Q

what happens when acetylcholine is released via exocytosis

A

binds on cholinoceptors (nicotinic + muscarinic)

when broken down, choline can be recycled and be transported back into the neuron through CHT, and acetate is released out

61
Q

true or false

Acetyl-CoA is synthesized in the cytoplasm

A

FALSE - in the mitochondria

acetylcholine is synthesized in the cytoplasm

62
Q

explain how acetycholine is stored in vesicles

A

vesicular ACh is bound to - charged VPG (vesicular proteoglycan)

these vesicles are on the inner surface of the nerve terminal by SNARE proteins that are on the vesicle (v-SNARES - synaptobrevin) and on the inside of the terminal cell membrane (t-SNARES - syntaxin and SNAP 25)

63
Q

the release of acetylcholine from the vesicle is dependent on…….

A

extracellular calcium. occurs when an action potential triggers the influx of calcium via N-type Ca channels

calcium interacts with VAMP synaptotagmins on the vesicle membrane which triggers the FUSION of the vesicle membrane with the terminal membrane.

a pore opnes into the synapse and cations rush in and acetylcholine is released via exocytosis into the synaptic cleft

64
Q

acetylcholine vesicle release is blocked by……

acetylcholine vesicle release is enhanced by…..

A

blocked by botulinum toxin

enhanced by black widow spider venom

65
Q

acetylcholine binds and activates…..

A

cholinoreceptor

66
Q

true or false

acetylcholine undergoes rapid deactivation by acetylcholinesterases

A

true

67
Q

what are other cholinesterases with a lower specificity for acetylcholine?

A

butyrylcholinesterase
(pseudocholinesterase)

68
Q
A

Pharmacology FINAL (11 decks)

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