elm 10.2

Question 1

what are some derivatives of barbiturates?

Answer 1

amobarbital
pentobarbital
thiopental
phenobarbital

Question 2

what are some historical uses of barbiturates?

Answer 2

anxiolytics
anticonvulsants
sedatives/hypnotics
anaesthetics

Question 3

barbiturates are positive ____ modulators of ____ receptors - they ____ the open time.

Answer 3

allosteric
GABAA
prolong

Question 4

at higher concentrations, barbiturates can directly _____ the receptor

Answer 4

activate

Question 5

barbiturates may also _____ AMPA receptors, ___ type VSCC (to inhibit ___ release)

Answer 5

inhibit
P/Q
NT

Question 6

thiopental is an ___ agent in general anaesthesia

Answer 6

induction

Question 7

thiopental can also be used in ___ when the seizure hasn’t responded to ___ or ____

Answer 7

status epileptus
benzodiazepines
anti-convulsants

Question 8

benzodiazepines are ______ allosteric modulators of the ____ receptor

Answer 8

positive
GABAA

Question 9

benzodiazepines are used as anxiolytics t or f

Answer 9

t

Question 10

GABA binding sites are formed at the interfaces of _____

Answer 10

beta

Question 11

high affinity BDZ binding requires a ___ subunit

Answer 11

gamma2

Question 12

what are some compounds that enhance GABAA receptor function

Answer 12

anxiolytic, sedative, muscle relaxant, amnesic, anticonvulsant

Question 13

what are some compounds that decrease GABAA receptor function

Answer 13

convulsants

Question 14

flumazenil is a benzodiazepine ____, which competes with agonists for the same binding site, but it is pharmacologically fairly ______. it is used to reverse _____

Answer 14

antagonist
inactive
BDZ sedation

Question 15

benzodiazepine inverse agonists - beta carbolines act at the same site as ______, and they ___ channel opening frequency

Answer 15

flunitrazepam
decrease

Question 16

high affinity is associated with type ____ benzodiazepine binding sites

Answer 16

I

Question 17

low affinity is associated with type ____ benzodiazepine binding sites

Answer 17

II

Question 18

what are two examples of early anxioselective BDZ ligands?

Answer 18

bretazenil
alpidem, ocinaplon

Question 19

what are 4 examples of behavioural tests

Answer 19

elevated plus maze
vogel water-lick conflict test
rotorod test
morris water maze

Question 20

what is the strategy for knockout studies

Answer 20

eliminate individual subunits from genome and to see if this alters sedative or anxiolytic properties of BDZs

Question 21

which subunit is related to cerebellar expression?

Answer 21

alpha 6

Question 22

which subunits are related to perinatally lethal ?

Answer 22

beta 3
gamma 2

Question 23

alpha one is type __

Answer 23

I

Question 24

alpha 2,3,5 is related to type __

Answer 24

II

Question 25

alpha 4,6 is realted to

Answer 25

high affinity

Question 26

mutation conserved alpha His to Arg in BDZ site leads to what

Answer 26

complete loss of classic BDZ binding

Question 27

knock in is what

Answer 27

in vivo replacement of single amino acid in a defined gene

Question 28

sedative, amnesic actions are

Answer 28

alpha 1

Question 29

anxiolytic actions are

Answer 29

alpha 2

Question 30

alpha 1 selective drugs would give you what

Answer 30

sleeping tablets

Question 31

alpha 2 selective drugs give you what

Answer 31

anti anxiety without sedation

Question 32

Which of the following barbiturates has been frequently used as an ingredient of lethal injections? a. Amobarbital b. Barbital c. Phenobarbital d. Thiopental

Answer 32

d

Question 33

Which subunit of the GABAA receptor contains the primary binding site for the barbiturates? a. Alpha b. Beta c. Delta d. Gamma 2

Answer 33

b

Question 34

The main current clinical uses of barbiturates are as: a. Anxiolytics and sedatives b. Anticonvulsants and anaesthetics (induction agents) c. Anxiolytics and anticonvulsants d. Muscle relaxants and anaesthesia (induction agents)

Answer 34

b

Question 35

Which alpha subunits confer high affinity binding for diazepam when they form a benzodiazepine binding site with the gamma 2 subunit? a. 1,2,3,5 b. 1,2,4,6 c. 2,4,5,6 d. 3,4,5,6

Answer 35

a

Question 36

Flumazenil is a _____________ of the GABAA receptor a. negative allosteric modulator b. non-competitive antagonist c. positive allosteric modulator d. silent allosteric modulator

Answer 36

d

Question 37

Which residue in alphas 1,2,3,5 confers high affinity binding for diazepam? a. G153 b. H105 c. R105 d. Y90

Answer 37

b

Question 38

Which of the following tests can be used to measure the amnesic actions of benzodiazepines? a. Elevated plus maze b. Morris water maze c. Rotorod test d. Vogel water lick conflict test

Answer 38

b