PHM 431 EXAM 1 QUESTIONS WITH
COMPLETE ANSWERS
Factors that contribute to drug addiction and continued drug use - Answer-drug
tolerance
drug dependence
drug withdrawal
The EC50 is a measure of drug: - Answer-potency
What brain area is not part of the mesolimbic dopamine system? - Answer-
hypothalamus
An inhibitor of the enzyme dopamine-beta-hydroxylase will reduce brain levels of which
of the following neurotransmitters? - Answer-norepinephrine
- dopamine is the precursor for norepinephrine synthesis catalyzed by dopamine-b-
hydroxylase
Charybdotoxin - Answer-blocks K+ channels which are required for the repolarization
phase of action potentials
GTP-gamma-S is a drug that irreversibly activates G-proteins. One effect of treating
neurons with this drug would be: - Answer-increased levels of intracellular cyclic 3', 5'
AMP
One consequence of "knockout" or deletion of the gene that encodes the enzyme
phenylethanolamine-N-methyl-transferase would be: - Answer-depletion of epinephrine
from the adrenal medulla
Drugs which inhibit acetylcholinesterase would enhance neurotransmission in which
brain region? - Answer-Septohippocampal neurons
- ACh is an important neurotransmitter in this brain area
Knockout of the gene that encodes the enzyme, monamine oxidase would result in
enhanced neurotransmission at which kind of synapse? - Answer-5-HT synapses
and
gamma-ammino-butyric acid (GABA)
Pargyline is a drug that inhibits the enzyme monoamine oxidase. This drug would be
expected to strength synaptic transmission at which kind of synapse? - Answer-
Norepinephrine synapses, dopamine and serotonin
Chloride - Answer-predominant intracellular anion
, What type of ion channel is responsible for the rising phase of an action potential? -
Answer-sodium channel
Most important inhibitory neurotransmitter in the CNS - Answer-gamma amino butyric
acid (GABA)
The GABAA receptor is a target for which of the following drug? - Answer-alcohol
What is a characteristic of the nicotinic acetylcholine receptor? - Answer-short latency to
activation
Adverse events caused by the drug cisapride was a primary reason for FDA
requirements of what drug screen? - Answer-HERG potassium channel activity
Phase 4 clinical trial - Answer-testing an already approved drug for a new indication
Gold standard for drug testing? - Answer-Double blind placebo controlled studies
What factor would NOT increase the risk that an individual will become addicted to a
drug or drugs - Answer-high level of plasma protein binding
BoTox is potentially lethal because: - Answer-it cleaves SNARE proteins required for
neurotransmitter release
Extracellular Cl- concentration is higher than the intracellular Cl- concentration. This Cl-
ion concentration gradient is needed for: - Answer-GABAa receptor signalling
traditional model of drug discovery - Answer-in-house research teams with expertise in
specific topic areas. Ex: cardiovascular diseases, diabetes, mental illness, inflammation,
cancer
New model of drug discovery - Answer-"big pharma" from smaller companies with a
narrow focus. big pharma purchases the rights to a drug after the start-up
existing drugs can motivate research on related drugs: treatment of peptic ulcer disease
- Answer-- development of H2 histamine receptor antagonists
- they "cured" ulcers, but if the patient stopped taking drug, ulcers would return
- Tagamet was the first billion dollar drug
- caused anti-androgenic affects and P450 inhibition
High throughput screening (HTS) - Answer-immortalized cell line expressing the
receptor or the other target
- cells loaded with a fluorescent molecule that emits light when activated
- calcium indicators
- 1:100 chance
COMPLETE ANSWERS
Factors that contribute to drug addiction and continued drug use - Answer-drug
tolerance
drug dependence
drug withdrawal
The EC50 is a measure of drug: - Answer-potency
What brain area is not part of the mesolimbic dopamine system? - Answer-
hypothalamus
An inhibitor of the enzyme dopamine-beta-hydroxylase will reduce brain levels of which
of the following neurotransmitters? - Answer-norepinephrine
- dopamine is the precursor for norepinephrine synthesis catalyzed by dopamine-b-
hydroxylase
Charybdotoxin - Answer-blocks K+ channels which are required for the repolarization
phase of action potentials
GTP-gamma-S is a drug that irreversibly activates G-proteins. One effect of treating
neurons with this drug would be: - Answer-increased levels of intracellular cyclic 3', 5'
AMP
One consequence of "knockout" or deletion of the gene that encodes the enzyme
phenylethanolamine-N-methyl-transferase would be: - Answer-depletion of epinephrine
from the adrenal medulla
Drugs which inhibit acetylcholinesterase would enhance neurotransmission in which
brain region? - Answer-Septohippocampal neurons
- ACh is an important neurotransmitter in this brain area
Knockout of the gene that encodes the enzyme, monamine oxidase would result in
enhanced neurotransmission at which kind of synapse? - Answer-5-HT synapses
and
gamma-ammino-butyric acid (GABA)
Pargyline is a drug that inhibits the enzyme monoamine oxidase. This drug would be
expected to strength synaptic transmission at which kind of synapse? - Answer-
Norepinephrine synapses, dopamine and serotonin
Chloride - Answer-predominant intracellular anion
, What type of ion channel is responsible for the rising phase of an action potential? -
Answer-sodium channel
Most important inhibitory neurotransmitter in the CNS - Answer-gamma amino butyric
acid (GABA)
The GABAA receptor is a target for which of the following drug? - Answer-alcohol
What is a characteristic of the nicotinic acetylcholine receptor? - Answer-short latency to
activation
Adverse events caused by the drug cisapride was a primary reason for FDA
requirements of what drug screen? - Answer-HERG potassium channel activity
Phase 4 clinical trial - Answer-testing an already approved drug for a new indication
Gold standard for drug testing? - Answer-Double blind placebo controlled studies
What factor would NOT increase the risk that an individual will become addicted to a
drug or drugs - Answer-high level of plasma protein binding
BoTox is potentially lethal because: - Answer-it cleaves SNARE proteins required for
neurotransmitter release
Extracellular Cl- concentration is higher than the intracellular Cl- concentration. This Cl-
ion concentration gradient is needed for: - Answer-GABAa receptor signalling
traditional model of drug discovery - Answer-in-house research teams with expertise in
specific topic areas. Ex: cardiovascular diseases, diabetes, mental illness, inflammation,
cancer
New model of drug discovery - Answer-"big pharma" from smaller companies with a
narrow focus. big pharma purchases the rights to a drug after the start-up
existing drugs can motivate research on related drugs: treatment of peptic ulcer disease
- Answer-- development of H2 histamine receptor antagonists
- they "cured" ulcers, but if the patient stopped taking drug, ulcers would return
- Tagamet was the first billion dollar drug
- caused anti-androgenic affects and P450 inhibition
High throughput screening (HTS) - Answer-immortalized cell line expressing the
receptor or the other target
- cells loaded with a fluorescent molecule that emits light when activated
- calcium indicators
- 1:100 chance
