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NSG 531 ADVANCED PHARMACOLOGY EXAM
How does alcohol inhibit the effects of long-term potentiation? - ANSWER
Alcohol has an inhibitory effect on NMDA receptors, which blocks the influx of
Na+ and Ca2+ (depolarizing currents). This also prevents some phosphorylation of
AMPA channels as the whole LTP pathway is dampened.
GABA is an ______ neurotransmitter that binds to ______ receptors. - ANSWER
inhibitory; GABA-A and GABA-B
GABA-A receptors are ligand-gated ion (ionotropic) channels selective for ______ .
- ANSWER Cl-
Common GABA-A agonist - ANSWER Propofol
Benzodiazepine works on ______ receptors. - ANSWER GABA-A; but it's not a
direct agonist. Binds to the modulatory region, resulting in an increased ability of
the channel to open when GABA binds. Allows more Cl- to flow inside, more
inhibition.
Flumazenil - ANSWER GABA-A antagonist used to reverse the effects of
benzodiazepines. Inhibits the effects of GABA so that less Cl- flows in.
GABA-B receptors are _______ that cause inhibition via _______ . - ANSWER G
protein-coupled receptors; beta unit breaks off and inhibits adenylyl cyclase OR
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directly binds to K+ (positive effect) or Ca2+ (negative effect) such that the cell
becomes hyperpolarized.
True or false: GABA-B receptors can be located on the presynaptic neurons that
release glutamate. - ANSWER True; GABA can spill over to nearby presynaptic
glutamate neurons, binds to GABA-B receptors there, and inhibit the further
release of glutamate.
Baclofen - ANSWER GABA-B receptor agonist and skeletal muscle relaxant. Binds
to GABA-B receptors on postsynaptic motor neurons and presynaptic excitatory
neurons that release glutamate.
True or false: norepinephrine and dopamine are both catecholamines with a
similar structure. - ANSWER True: both have a benzene ring and two hydroxyl
groups.
Norepinephrine is released from the _____ in the CNS. - ANSWER locus ceruleus
(part of the brainstem involved in stress and panic responses)
Problems with tricyclic antidepressants - ANSWER Block re-uptake transporters
for NE, with the previous theory that depression was caused by a depletion of
catecholamines. But, they have a low sensitivity for NE, and also block the
reuptake of serotonin (leading to serotonin syndrome) and histamine (causes
sedation), and block postsynaptic muscarinic receptors for ACh (causing
anticholinergic effects).
Dopamine is largely produced from cells in the ______ . - ANSWER substantia
nigra and ventral tegmental area of the brain; then travels to the mesolimbic
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system (reward system, regulation of affect) and pathways that extend to the
prefrontal cortex (effects on thinking and judgement)
True or false: there are 5 known subtypes of dopamine receptors. - ANSWER True
Effects of cocaine - ANSWER Blocks the reuptake of dopamine AND
norepinephrine in presynaptnic neurons, leading to a sense of reward and
pleasure, but also heightened sense of arousal and dangerous CV effects.
How do first-generation antipsychotics (Haldol, thorazine) improve symptoms of
schizophrenia? What are the undesirable side effects? - ANSWER As dopamine
receptor (D2) antagonists, they block the effects of dopamine in the cerebral
cortex, leading to desired behavioral changes. However, they also block the effects
of dopamine in the mesolimbic system (changes in affect) and the basal ganglia
and cerebellum (undesirable motor effects, tremors and shuffling gait).
How are the newer, atypical antipsychotics an improvement over first-generation?
- ANSWER 1) they block both dopamine and serotonin (D2, 5HT2) receptors -
serotonin is associated with schizophrenia. 2) have faster on-off D2 kinetics to get
desirable effects in the cortex, but avoid indesirable effects in the mesolimbic
system, basal ganglia, and cerebellum.
What imbalance of neurotransmitters causes typical Parkinson's Disease
symptoms? - ANSWER A depletion of dopamine (inhibitory effects on movement)
resulting in a relative increase of acetylcholine (excitatory effects on movement).
Why is the pharmacologic management of Parkinson's Disease so challenging? -
ANSWER Dopamine isn't lipid soluble, so we give a precursor, l-dopa. There are
NSG 531 ADVANCED PHARMACOLOGY EXAM
How does alcohol inhibit the effects of long-term potentiation? - ANSWER
Alcohol has an inhibitory effect on NMDA receptors, which blocks the influx of
Na+ and Ca2+ (depolarizing currents). This also prevents some phosphorylation of
AMPA channels as the whole LTP pathway is dampened.
GABA is an ______ neurotransmitter that binds to ______ receptors. - ANSWER
inhibitory; GABA-A and GABA-B
GABA-A receptors are ligand-gated ion (ionotropic) channels selective for ______ .
- ANSWER Cl-
Common GABA-A agonist - ANSWER Propofol
Benzodiazepine works on ______ receptors. - ANSWER GABA-A; but it's not a
direct agonist. Binds to the modulatory region, resulting in an increased ability of
the channel to open when GABA binds. Allows more Cl- to flow inside, more
inhibition.
Flumazenil - ANSWER GABA-A antagonist used to reverse the effects of
benzodiazepines. Inhibits the effects of GABA so that less Cl- flows in.
GABA-B receptors are _______ that cause inhibition via _______ . - ANSWER G
protein-coupled receptors; beta unit breaks off and inhibits adenylyl cyclase OR
,2|Page
directly binds to K+ (positive effect) or Ca2+ (negative effect) such that the cell
becomes hyperpolarized.
True or false: GABA-B receptors can be located on the presynaptic neurons that
release glutamate. - ANSWER True; GABA can spill over to nearby presynaptic
glutamate neurons, binds to GABA-B receptors there, and inhibit the further
release of glutamate.
Baclofen - ANSWER GABA-B receptor agonist and skeletal muscle relaxant. Binds
to GABA-B receptors on postsynaptic motor neurons and presynaptic excitatory
neurons that release glutamate.
True or false: norepinephrine and dopamine are both catecholamines with a
similar structure. - ANSWER True: both have a benzene ring and two hydroxyl
groups.
Norepinephrine is released from the _____ in the CNS. - ANSWER locus ceruleus
(part of the brainstem involved in stress and panic responses)
Problems with tricyclic antidepressants - ANSWER Block re-uptake transporters
for NE, with the previous theory that depression was caused by a depletion of
catecholamines. But, they have a low sensitivity for NE, and also block the
reuptake of serotonin (leading to serotonin syndrome) and histamine (causes
sedation), and block postsynaptic muscarinic receptors for ACh (causing
anticholinergic effects).
Dopamine is largely produced from cells in the ______ . - ANSWER substantia
nigra and ventral tegmental area of the brain; then travels to the mesolimbic
, 3|Page
system (reward system, regulation of affect) and pathways that extend to the
prefrontal cortex (effects on thinking and judgement)
True or false: there are 5 known subtypes of dopamine receptors. - ANSWER True
Effects of cocaine - ANSWER Blocks the reuptake of dopamine AND
norepinephrine in presynaptnic neurons, leading to a sense of reward and
pleasure, but also heightened sense of arousal and dangerous CV effects.
How do first-generation antipsychotics (Haldol, thorazine) improve symptoms of
schizophrenia? What are the undesirable side effects? - ANSWER As dopamine
receptor (D2) antagonists, they block the effects of dopamine in the cerebral
cortex, leading to desired behavioral changes. However, they also block the effects
of dopamine in the mesolimbic system (changes in affect) and the basal ganglia
and cerebellum (undesirable motor effects, tremors and shuffling gait).
How are the newer, atypical antipsychotics an improvement over first-generation?
- ANSWER 1) they block both dopamine and serotonin (D2, 5HT2) receptors -
serotonin is associated with schizophrenia. 2) have faster on-off D2 kinetics to get
desirable effects in the cortex, but avoid indesirable effects in the mesolimbic
system, basal ganglia, and cerebellum.
What imbalance of neurotransmitters causes typical Parkinson's Disease
symptoms? - ANSWER A depletion of dopamine (inhibitory effects on movement)
resulting in a relative increase of acetylcholine (excitatory effects on movement).
Why is the pharmacologic management of Parkinson's Disease so challenging? -
ANSWER Dopamine isn't lipid soluble, so we give a precursor, l-dopa. There are