neuropharm last lec Flashcards

1
Q

Neuropharm test 2 last lec

what is the structural of nACh receptors?

A

_ at least 2 alpha subunits
_ hill coefficient = 2 (requires at least 2 Ach molecule to activate)
_ do not hyperpolarize neurons
o calcium channel (inward current _ depolarize

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2
Q

Neuropharm test 2 last lec

how does nAch receptor open or close its gate ?

A

via conformational change
_ General conformational change

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3
Q

Neuropharm test 2 last lec

how does nAch receptor change their conformation?

A

_ Subunits rotate relative to one another to open/close channel

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4
Q

Neuropharm test 2 last lec

what structure is unique in torpedo fish?

A

their nicotinic receptor in their electroplax organ which produces a large bolt of electrical current and stun every fish around them

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5
Q

Neuropharm test 2 last lec

what is different of the nicotinic channel in Torpedo fish and human?

A

the torpedo fish have gram worth of these channels which alow them for the massive electrical current

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6
Q

Neuropharm test 2 last lec

what subunit is specific to nAch receptors?

A

the alpha subunit of them which makes them nAch receptors

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7
Q

Neuropharm test 2 last lec

how does subunit of nAch receptors different in different region?

A

alpha subunit is all over the nervous system, beta-2 are all over the place, 3 only in selective places, 4 is found in Habinula

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8
Q

Neuropharm test 2 last lec

how does these subunit change with againg?

A

Alpha, beta and delta are the ones sen in asult. Early in life instead of delta we had Gamma subunit. We also had Epsilon early in life

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9
Q

Neuropharm test 2 last lec

where are these subunit found?

A

_ researched showed they were located pre- and post-synapticall. they are also found elsewhere on the axon (pre-terminally _ axolemnal locations)

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10
Q

Neuropharm test 2 last lec

how is the overal Hill coeficient of nAChR receptors?

A

More nAChR diversity, Different Hill coefficients

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11
Q

Neuropharm test 2 last lec

what is the relationship of nAChR alpha 7 receptors and smoking?

A

requirement to activate the receptors seems to go down with experience to nicotine

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12
Q

Neuropharm test 2 last lec

what kind of sununits are used in Alpha 7 receptors?

A

theyahve all 5 subunits identical

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13
Q

Neuropharm test 2 last lec

how does nicotinic receptors or nAChR alpha 7 receptors affext the expression and glucose utilization?

A

low-level of expression in non-smokers. nonsmokers show high levels of glucose utilization. utilization of glucose goes down the more they smoke _ possible calming effect

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14
Q

Neuropharm test 2 last lec

what is th effect of nAChR of Na?

A

nAChR mediate the Na+ current

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15
Q

Neuropharm test 2 last lec

what is the nAChRhill coefficient?

A

most of these receptors have Hill coefficient of 2 (1 is not sufficient

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16
Q

Neuropharm test 2 last lec

what are the uses of nAChR ligands clinically?

A

o Treatment of: 1-Motor dysfunctions. 2-Cognitive impairments, ADD. 3-Memory impairments. 2-Tobacco addiction. 3- Autonomic functions 4- Surgical paralysis

17
Q

Neuropharm test 2 last lec

what are the non-clinical use of nAChR ligands?

A

o Recreational Smoking, chewing, snuff, Insecticides, neurotoxins, Paralytic, assassination poisons

18
Q

Neuropharm test 2 last lec

what are some of the Short and long-acting analogs of Ach?

A

1-ACh (endogenous ligand): Broken down extremely rapidly after release from pre-synaptic terminals
2-Shortest acting analog: Carbachol _ lasts much longer than ACh in the synapse

19
Q

Neuropharm test 2 last lec

where are the 3 region of the body where we look for nAchR?

A

CNS, autonmic ganglia, NMJ

20
Q

Neuropharm test 2 last lec

what kind of subunit of n-AchR is only in mostly in brain or CNS?

A

Alpha-7

21
Q

Neuropharm test 2 last lec

what are the competitive agonist that works on CNS, autonomic ganglia and NMJ?

A

Ach, Carbachol, Nicotine

22
Q

Neuropharm test 2 last lec

which one of the competitive agonist does not work on autonomic ganglia but it does on all other area?

A

Anatoxin

23
Q

Neuropharm test 2 last lec

which kind of agonist is specific to autonomic ganglia?

A

DMPP

24
Q

Neuropharm test 2 last lec

which kind of agonist is specific to NMJ?

A

Suxamethonium

25
Q

Neuropharm test 2 last lec

which kind of agonist is specific to CNS only?

A

Labeline, Anabasine

26
Q

Neuropharm test 2 last lec

what is the endogenous agonist that works on all regions?

A

Ach

27
Q

Neuropharm test 2 last lec

for the non-alpha7 CNS name an competitive antagonist?

A

Coronaridine

28
Q

Neuropharm test 2 last lec

for the alpha-7 CNS which name a competitive antagonist?

A

Alpha-bungarotoxin _ competitive antagonist

29
Q

Neuropharm test 2 last lec

which none-competitive antagonist block alpha-7 CNS?

A

Buproprion (wellbutrin) _ noncompetitive antagonist

30
Q

Neuropharm test 2 last lec

what is an competitve antagonist of autonomic ganglia?

A

Hexamethonium, kappa-bungarotoxin

31
Q

Neuropharm test 2 last lec

which antagonist keeps the membane of the Autonomic ganglia depolarized?

A

Trimethaphan (technically very, very strong agonists)

32
Q

Neuropharm test 2 last lec

what are some of the competitive antagonist for NMJ nAChR?

A

Decamethonium, curare, tubocurarine (active compound)

33
Q

Neuropharm test 2 last lec

what is the name of the depolarizing agonist for NMJ nAChR ?

A

Succinylcholine _ depolarizing blocker (keeps membrane depolarized

34
Q

Neuropharm test 2 last lec

what are some of the non-competitive antagonist of CNS, CNS alpha 7, autonomic ganglia, NMJ?

A

PCP, TEA

35
Q

Neuropharm test 2 last lec

name a suicide antagonist for CNS, CNS alpha 7, AG, NMJ?

A

bromoACh

36
Q

Neuropharm test 2 last lec

what are some of the hexamethonium and it family?

A

o 6 hydro carbons, fairly specific for ganglionic receptors, shorter the drugs are, the more specific they are for the ganglionic
the longer version is more specific for Ach receptor

37
Q

Neuropharm test 2 last lec

how can neuro-transmission be altered?

A

_ Nerve AP
_ Biosynthesis
_ Vesicular release
_ Receptors
_ Degradation
_ Ion channels
_ Spread of muscle excitation
_ Muscle contration