subtypes of GABAaR's

Question 1

what does anticonvulsant do

Answer 1

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

Question 2

what is an analgesic drug

Answer 2

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

Question 3

what is an amnesic drug

Answer 3

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

Question 4

drugs that enhance GABAaR function can be described as what

Answer 4

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

Question 5

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

Answer 5

impair cognition, produce tolerance, and become addictive

Question 6

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

Answer 6

benzodiazepines

Question 7

what are benzodiazepines used to treat

Answer 7

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

Question 8

what are some side affects of benzodiazepines

Answer 8

induce muscle contraction
can produce amnesia

Question 9

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

Answer 9

within weeks tolerance can develop and addiction may occur

Question 10

what is a PAM

Answer 10

positive allosteric modulator

Question 11

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

Answer 11

PAM
NAM
antagonist

Question 12

what is a NAM

Answer 12

negative allosteric modulator

Question 13

what is the action of an antagonist of GABAaR

Answer 13

do not influence GABAaR but prevent action of PAMs or NAMs

Question 14

what is the action of PAMs on the GABAaR

Answer 14

enhance function

Question 15

what is the action of NAMs on the GABAaR

Answer 15

decrease function

Question 16

what are some example of PAMs

Answer 16

diaepam, flunitrazepam

Question 17

what are some examples of NAMs

Answer 17

DMCM
a Beta carboline

Question 18

what is an example of an antagonist of the GABAaR

Answer 18

Flumazenil

Question 19

where do benzodiazepines bind on the GABAaR

Answer 19

between the interface of the alpha and gamma subunit of GABAaR

Question 20

what are the subunits of GABAaR

Answer 20

alpha x2
beta x2
gamma x1

Question 21

what ion flows through the central pore of GABAaRs

Answer 21

Cl-

Question 22

what are the affects of PAMs

Answer 22

anxiolytic, sedative, analgesic, anticonvulsant

Question 23

what are the effects of NAMs

Answer 23

pro convulsant, anxiogenic

Question 24

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

Answer 24

alpha1beta1

Question 25

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

Answer 25

gamma2

Question 26

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

Answer 26

gamma - but usually gamma2

Question 27

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

Answer 27

gamma2 AND alpha1, alpha2, alpha3, or alpha5

Question 28

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

Answer 28

gamma 2 AND alha6 or alpha 4

Question 29

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

Answer 29

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

Question 30

mutations of R101 to H produces a diazepam _______ receptor

Answer 30

sensitive

Question 31

mutation of alpha1H101 to R does what to diazepam sensitivity

Answer 31

blocks diazepam sensitivity

Question 32

an alpha1/alpha6 chimera can do what

Answer 32

diazepam sensitive

Question 33

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

Answer 33

autoradiography

Question 34

alpha1H101R mouse autoradiography reveals the alpha1 mutation to cause what

Answer 34

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

Question 35

in the alpha1H101R mouse, what effects are blunted

Answer 35

sedative

Question 36

sedative effects are not impaired in what mouse

Answer 36

alpha2H101R mouse

Question 37

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

Answer 37

alpha1H101R mouse alpha2H101R mouse

Question 38

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

Answer 38

myorelaxant

Question 39

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

Answer 39

alpha1H101R mouse

Question 40

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

Answer 40

alpha1betagamma2

Question 41

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

Answer 41

alpha1H101R

Question 42

the anxiolytic effects of diazepam are mediated by what GABAaRs

Answer 42

alpha2betagamma2

Question 43

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

Answer 43

are mediated by alpha2betagamma2 are not mediated by alpha1betagamma2

Question 44

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

Answer 44

alpha2H101R

Question 45

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

Answer 45

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

Question 46

in what mouse is diazepam no longer anxiolytic but is sedative

Answer 46

alpha2H101R mouse

Question 47

in what mouse is diazepam no loner sedative but is anxiolytic

Answer 47

alpha1H101R mouse

Question 48

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

Answer 48

alpha1

Question 49

L-838,417 is anxiolytic but not ______

Answer 49

sedative

Question 50

L-838,417 is ______ but not sedative

Answer 50

anxiolytic