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biomembranes > CYS loop receptors > Flashcards

CYS loop receptors Flashcards

1
Q

what are CYS-loop receptors

A

ligand gated ion channels

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2
Q

how many protein subunits make up a Cys-loop receptor

A

5 (pentamer)

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3
Q

define homo-oligimer

A

same subunit type

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4
Q

define hetero-oligimer

A

different types of subunits

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5
Q

where is the ligand binding site on nAChR

A

between subunit interfaces

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6
Q

what is the role of the Ach binding protein

A

takes up extra ACh

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7
Q

what ions are each receptors permeable to

A

K Na Ca

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8
Q

nAChRs are _________ ______________ channels

A

non specific cation

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9
Q

what does cation mean

A

positively charged ion

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10
Q

what does nAChRs modulate

A

fast synaptic excitation

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11
Q

What are some key members of the Cys-loop receptor family?

A

nAChRs
GABA(A) receptors
glycine receptors
5-HT3 receptors

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12
Q

name a autoimmune disorder associated with loss of nAChRs at neuromuscular junction

A

myasthenia Gravis

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13
Q

how is myasthenia Gravis diagnosed

A

typically through a blood test for antibodies of nAChRsn

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14
Q

name reversible competitive antagonists of AChE

A

neostigmine
pyridostigmine
edrophonium

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15
Q

what is congenital myasthenia syndrome

A

neuromuscular disorder caused by defects of several types at the neuromuscular junctionmutations that affect each receptor expression

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16
Q

name drugs that act as agonists on nAChRs

A

acetylcholine
nicotine
vareniciline

17
Q

name a partial agonist for nAChR

A

varenicline

18
Q

what is the main nAChR in the brain

A

a4B2

19
Q

5-HT3 is permeable to which ions

A

Na K Ca

20
Q

5-HT3 is a _________ _____________ channels
and modulate?

A

non-specific cation
fast synaptic excitation

21
Q

how doe the structure of 5-HT3 compare to nAChR

A

identical

22
Q

where are 5-HT3 receptors greatly expressed
and they modelate?

A

gut
peristalsis

23
Q

name 5-HT3 receptor antagonists

A

anti-emetic drugs
eg. sterones (ondansetron)

24
Q

name a target for positive allosteric modulators

A

GABA(A) receptor

25
Q

name a neuro steriod allosteric modulator

A

allopregnanolone

26
Q

what are benzodiazepines

A

positive allosteric modulators of synaptic GABA A receptors

27
Q

mechanism of action of benzodiazepines

A

enhance GABA at GABA A receptor, increasing channel opening frequency causing a greater flux of Cl inside the cell so create a resistance to excitation
therefore slows down brain activity

28
Q

what are benzodiazepines used to treat

A

anxiety
sleep disorders
epilepsy

29
Q

name some common benzodiazepines

A

diazepam (long half life)
lorazepam (short half life)
midazolam (short half life)

30
Q

how does propofol work as a anaesthetic

A

binds to a1B3y2 GABA A receptors
this generates a Cl influx hyperpolarisong the cell inhibiting AP and synaptic transmission

31
Q

name anaesthetics that are positive allosteric modulators of GABA A receptor

A

thiopental
etomidate
propofol

32
Q

the drugs that are non-bento hypnotics are positive allosteric modulators of GABA A receptors are known as

A

Z drugs
zolpidem
zopiclone
zaleplon

33
Q

how do pregnant steroids relate to GABA A receptors

A

they are allosteric positive modulators of GABA A receptors

34
Q

allosteric modulators of GABA A have what effect on channels

A

increase the opening time of the channels

35
Q

how can neurosteriod levels be altered

A

alcohol and some SSRI antidepressants

36
Q

neurosteriods can act at very ____ concentrations

A

low

37
Q

give an example of a cell that has extra synaptic GABA A receptor

A

glial cells

38
Q

synaptic GABA A receptors are __________ conductance

A

phasic

39
Q

__________ conductance is mediated by activation of ?

A

tonic
extra-synaptic receptors

biomembranes (11 decks)

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