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Behavioral Neuroscience and Pharmacology > subtypes of GABAaR's > Flashcards

subtypes of GABAaR's Flashcards

1
Q

what does anticonvulsant do

A

Anticonvulsant drugs are medicines used to prevent or treat convulsions (seizures)

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2
Q

what is an analgesic drug

A

An analgesic drug is a pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain

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3
Q

what is an amnesic drug

A

Drug-induced amnesia is intentionally caused by injection of an amnestic drug to help a patient forget surgery

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4
Q

drugs that enhance GABAaR function can be described as what

A

anxiolytic, anticonvulsant, analgesic, amnestic, sedative, hypnotic, and anaesthetic

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5
Q

However, drugs that can enhance GABAaRs function also have what cons

A

impair cognition, produce tolerance, and become addictive

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6
Q

what type of drugs are used to treat anxiety, insomnia, that also induce muscle contraction and control some forms of epilepsy and can produce amnesia

A

benzodiazepines

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7
Q

what are benzodiazepines used to treat

A

used to treat anxiety and insomnia
also used to treat some forms of epilepsy

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8
Q

what are some side affects of benzodiazepines

A

induce muscle contraction
can produce amnesia

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9
Q

why should you be careful when prescribing benzodiazepines in vulnerable individuals with compulsive drug use

A

within weeks tolerance can develop and addiction may occur

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10
Q

what is a PAM

A

positive allosteric modulator

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11
Q

what are the three names given to ligans when they act on the benzodiazepines site of a GABAaR

A

PAM
NAM
antagonist

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12
Q

what is a NAM

A

negative allosteric modulator

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13
Q

what is the action of an antagonist of GABAaR

A

do not influence GABAaR but prevent action of PAMs or NAMs

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14
Q

what is the action of PAMs on the GABAaR

A

enhance function

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15
Q

what is the action of NAMs on the GABAaR

A

decrease function

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16
Q

what are some example of PAMs

A

diaepam, flunitrazepam

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17
Q

what are some examples of NAMs

A

DMCM
a Beta carboline

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18
Q

what is an example of an antagonist of the GABAaR

A

Flumazenil

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19
Q

where do benzodiazepines bind on the GABAaR

A

between the interface of the alpha and gamma subunit of GABAaR

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20
Q

what are the subunits of GABAaR

A

alpha x2
beta x2
gamma x1

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21
Q

what ion flows through the central pore of GABAaRs

A

Cl-

22
Q

what are the affects of PAMs

A

anxiolytic, sedative, analgesic, anticonvulsant

23
Q

what are the effects of NAMs

A

pro convulsant, anxiogenic

24
Q

Diazepam does not enhance GABA responses mediated by GABAaR’s composed of what subunits

A

alpha1beta1

25
Q

Diazepam does not enhance the GABA responses mediated by GABAaR’s composed of alpha1beta1 but does for equivalent GABAaR’s containing what subunit

A

gamma2

26
Q

For high affinity binding of diazepam the receptor must contain what subunit

A

gamma - but usually gamma2

27
Q

GABAaR’s incorporating the gamma 2 and what alpha subunits are diazepam SENSITIVE

A

gamma2 AND
alpha1, alpha2, alpha3, or alpha5

28
Q

GABAaR’s incorporating the gamma2 and what alpha units are diazepam INSENSITIVE

A

gamma 2 AND
alha6 or alpha 4

29
Q

diazepam enhances function of alpha1, alpha2, alpha3 and alpha5 but not alpha4 or alpha6 GABAaR’s - why?

A

alpha,1,2,3,5 have a H residue at position 101
whereas both alpha4,6 subunits have a R residue at this position

30
Q

mutations of R101 to H produces a diazepam _______ receptor

A

sensitive

31
Q

mutation of alpha1H101 to R does what to diazepam sensitivity

A

blocks diazepam sensitivity

32
Q

an alpha1/alpha6 chimera can do what

A

diazepam sensitive

33
Q

the alpha1H101R mouse
what experiment reveals the alpha1 mutation to cause loss of 3H-flumazenil binding in the areas known to express the alpha1 subunit

A

autoradiography

34
Q

alpha1H101R mouse
autoradiography reveals the alpha1 mutation to cause what

A

a loss of 3H-flumazenil binding in areas known to express the alpha1 subunit

35
Q

in the alpha1H101R mouse, what effects are blunted

A

sedative

36
Q

sedative effects are not impaired in what mouse

A

alpha2H101R mouse

37
Q

sedative effect blunted = ________mouse
sedative effects not impaired in = ________ mouse

A

alpha1H101R mouse
alpha2H101R mouse

38
Q

the sedative effects are blunted in the alpha1H101R mouse but what effect is not affected

A

myorelaxant

39
Q

sedative effects are impaired in this mouse but the myorelaxant affects are not
what mouse is this

A

alpha1H101R mouse

40
Q

the anxiolytic effects of diazepam are NOT mediated by what type of GABAaRs

A

alpha1betagamma2

41
Q

diazepam incraeses the time spent in the light compartment (light/dark box) these effects do occur in what mouse

A

alpha1H101R

42
Q

the anxiolytic effects of diazepam are mediated by what GABAaRs

A

alpha2betagamma2

43
Q

the anxiolytic effects of diazepam are:
mediated by _____ GABAaRs
not mediated by ______ GABAaRs

A

are mediated by alpha2betagamma2
are not mediated by alpha1betagamma2

44
Q

diazepam increases the time spent in the light compartment (light/dark box) these effects of diazepam do not occur in what mice

A

alpha2H101R

45
Q

diazepam increases time spent on the open arms of the elevated plus maze
the effects do not occur in the _____ mouse
the effects do occur in the ______ mouse

A

do not occur in the alpha2H101R mouse
do occur in the alpha1H101R mouse

46
Q

in what mouse is diazepam no longer anxiolytic but is sedative

A

alpha2H101R mouse

47
Q

in what mouse is diazepam no loner sedative but is anxiolytic

A

alpha1H101R mouse

48
Q

L-838,417 potentiates GABA acting at alpha2, 3, and 5 but not at what alpha_ subunit containing receptors

A

alpha1

49
Q

L-838,417 is anxiolytic but not ______

A

sedative

50
Q

L-838,417 is ______ but not sedative

A

anxiolytic

Behavioral Neuroscience and Pharmacology (6 decks)

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