Quiz Flashcards
Which is a pre-condition for central action of a drug?
a. Lipophobic properties
b. Passage through the BBB and interaction with central structures like receptors
c. Increasing adrenaline levels significantly
d. Lowering membran potential
e. Boosting GABAergic function
b. Passage through the BBB and interaction with central structures like receptors
Which class does not belong to the antidepressants?
a. Specific serotonin reuptake inhibitors
b. Monoamine oxidase inhibitors
c. Psychostimulants
d. Butyrophenones
e. Non-selective noradrenaline-serotonine reuptake inhibitors
d. Butyrophenones
Which of these statements about ligands is correct?
a. A partial agonist gives a partial effect because it is only one part of the full agonist.
b. Antagonists do not change the response of a receptor.
c. Partial agonists evoke stronger responses than full agonists.
d. Full agonists bind more tightly than inverse agonists.
e. A full agonist can displace a partial agonist that is bound to a receptor.
b. Antagonists do not change the response of a receptor.
Randomisation
a. is a good substitue for a more thorough statistical analysis
b. amplifies otherwise small effects between control and test groups
c. removes sources of bias, even those that are not known
d. is appropriate experiments on ligand gated ion channels, but not for those on metabotropic receptors
e. is done after the experiment by analysing the data in a random order
c. removes sources of bias, even those that are not known
Dopaminergic drugs in Parkinsons disease do not
a. Promote dopamine synthesis
b. Decrease acetylcholine levels by competetive mechanisms
c. Prevent dopamine degradation
d. Promote dopamine release
e. Act as receptor agonists at D2-receptors alone
b. Decrease acetylcholine levels by competetive mechanisms
An indirectly acting parasympathomimetic drug acts
a. Blocking acetylcholine release
b. Selective at muscarinergic receptors
c. Increasing acetycholine levels in the synaptic cleft
d. Lowering adrenaline levels significantly
e. Boosting GABAergic function
c. Increasing acetycholine levels in the synaptic cleft
What are the differences between plasma membrane transporters and vesicular transporters for neurotransmitters?
[Please mark the correct statement(s)]
a. Plasma membrane transporters are vesicular transporters after the vesicle and cell membrane have fused. This is the reason for their high substrate specificity. They just use the Na+ instead of Cl- gradient to transport neurotransmitter molecules.
b. Plasma membrane transporters use the pH gradient to clear the synaptic cleft from the released neurotransmitter. Vesicular transporters use the Na+ gradient to pump neurotransmitter molecules into synaptic vesicles.
c. They are differentially spliced products of the same genes. This ensures high substrate specificity. Plasma membrane transporters mainly use Na+ gradients, as opposed to vesicular transporters which use pH gradients.
d. Plasma membrane transporters use the Na+ gradient to clear the synaptic cleft of the released neurotransmitter. Vesicular transporters use (among others) a pH gradient to pump neurotransmitter molecules into synaptic vesicles.
e. Vesicular transporters have a high substrate specificity and use a pH gradient as energy source. Plasma membrane transporters recognize the specific carboxyl group that all neurotransmitters share and therefore clear all neurotransmitters from the synaptic cleft.
d. Plasma membrane transporters use the Na+ gradient to clear the synaptic cleft of the released neurotransmitter. Vesicular transporters use (among others) a pH gradient to pump neurotransmitter molecules into synaptic vesicles.
Which central acting drugs are central stimulative?
a. Analeptics
b. anticonvulsants
c. sedatives
d. Anxiolytics
e. neuroleptics
a. Analeptics
The neurotransmitters in the autonomous nervous system are
a. Acetylcholine + dopamine
b. Glutamate + GABA
c. Acetylcholine + serotonine
d. Acetylcholine + noradrenaline
e. Serotonine + noradrenaline
d. Acetylcholine + noradrenaline
Which of the following statement(s) is/are correct?
a. Glutamate is synthesized in the soma and packed into vesicles which are transported to the synapse. The source of Glutamate is Tyrosine, which is decarboxylated and than aromatized by specific enzymes in the trans-Golgi network.
b. Neurons don’t synthesize Glutamate at all, but depend entirely on supply by Glial cells
c. Glutamate concentration in the cerebrospinal fluid is high and it can be taken up directly
d. There are 2 main sources for Glutamate, -ketoglutarate taken from the Krebs-cycle and Glutamine, which is partially delivered by glia cells.
e. Glutamate is an essential amino acid, it has to be included in the diet and is taken up directly into the blood stream which delivers it through the blood brain barrier to the brain.
d. There are 2 main sources for Glutamate, -ketoglutarate taken from the Krebs-cycle and Glutamine, which is partially delivered by glia cells.
Which of the following statement(s) is/are correct?
a. GABA is synthesized directly from Glutamate via Glutamatedecarboxylase (GAD). Only one isoform of this enzyme exists, GAD65
b. GABA is synthesized directly from Glutamate via Glutamatedecarboxylases.
Two Isoforms of this enzyme exist, GAD65 and GAD67.
c. GABA is synthesized directly by deamination of Glutamine, which is either produced in the Krebs cycle or delivered by glial cells.
d. GABA is synthesized directly from Glutamate via Glutamatedecarboxylases.
Two Isoforms of this enzyme exist, GAD32 and GAD69.
e. Isoleucine is the immediate precursor of GABA. The needed de-methylation is carried out by Isoleucine demethylases 65 and 95, yielding the important metabolite SAM.
b. GABA is synthesized directly from Glutamate via Glutamatedecarboxylases.
Two Isoforms of this enzyme exist, GAD65 and GAD67.
An ideal agonist will
a. not influence the ratio of inactive to active state of the receptor
b. shift the ratio in favor of the active state
c. shift the ratio in favor of the inactive state
d. fix the ratio of inactive to active receptor at a given, agonist specific value
b. shift the ratio in favor of the active state
Which of these statements about agonists is correct?
a. A partial agonist gives a partial effect because it is only one part of the full agonist
b. Inverse agonists do not change the response of a receptor
c. Full agonists evoke stronger responses than partial agonists
d. Full agonists bind more tightly than inverse agonists
e. A full agonist can displace a partial agonist that is bound to a receptor
c. Full agonists evoke stronger responses than partial agonists
Which of these statements about the Schild Method is false?
a. The Schild method requires binding to be at equilibrium.
b. The Schild method cannot estimate the number of binding sites in a receptor.
c. The Schild method provides a microscopically correct estimate of the binding affinity of a competitive antagonist.
d. The Schild method is appropriate for ligand gated ion channels, but not for metabotropic receptors.
e. The affinity of the agonist used does not affect the antagonist KB determined by Schild’s method.
d. The Schild method is appropriate for ligand gated ion channels, but not for metabotropic receptors.
A true competitive antagonist …
a. … blocks receptor activity by causing an irreversible conformational change
b. … cannot bind to all the sites on a receptor at the same time
c. … has a dissociation constant (KB) that is directly proportional to the IC50 value determined from an inhibition curve
d. … is the only type of drug whose microscopic dissociation constant cannot be estimated directly
e. … binds to the same site as an agonist but does not cause a conformational change that can activate the receptor
e. … binds to the same site as an agonist but does not cause a conformational change that can activate the receptor
Muscle relaxants do not
a. Act as agonists at the neuro-muscular junction
b. Depolarize the mebrane
c. Relax Skeletal muscle
d. Induce anaesthesia
e. Have adverse drug effects
d. Induce anaesthesia
Benzodiazepines do not
a. Influence GABAergic function
b. Have antiepileptic effects
c. Have a wide therapeutic range
d. Induce Cognitive Improvement
e. Reduce anxiety
d. Induce Cognitive Improvement
In the autonomous nervous system nicotine is
a. Dose-dependently an agonist and a blocker at the nicotinergic ganglia
b. Just an antagonist without effects
c. An agonist at muscarinergic receptors
d. An agonist at the ganglia, but a blocker of the neuromuscular junction
a. Dose-dependently an agonist and a blocker at the nicotinergic ganglia
Computational drug design
a. is a waste of time because nothing that is better than a natural product could ever be designed.
b. is mature and can replace all wet experiments.
c. allows the identification of promising novel therapeutic agents that can be refined with other methods.
d. cannot be used to find therapies that will cross the blood brain barrier, because this structure is too complicated to simulate.
e. only works if you want to design lipophilic molecules.
c. allows the identification of promising novel therapeutic agents that can be refined with other methods.
Glutamate receptors are amongst the best understood receptors in terms of mechanisms of activation because
a. numerous co-crystals of the ligand binding domain with a range of agonists and antagonists have been published
b. the crystal structure of the full length receptor revealed a single glutamate binding site
c. glutamate acts at only one class of receptors, making it easy to work out all the details
d. each subtype is only expressed in a few cells in the brain
e. they are surprisingly simple molecules, consisting of only a single transmembrane helix
a. numerous co-crystals of the ligand binding domain with a range of agonists and antagonists have been published
What energy sources do plasma membrane transporters of neurotransmitters mainly use?
a. Na+ gradient across the membrane
b. pH gradient
c. Free inorganic phosphate antiport
d. Glucose co-transport
Transport along their concentration gradient
a. Na+ gradient across the membrane
100% bioavailability is by definition achieved by:
a. intravenous
b. oral
c. rectal
d. intramuscular
e. inhalation
f. percutaneous
a. intravenous
Neurotransmitter activity can be terminated by:
a. Enzymatic inactivation in the synaptic cleft only
b. Enzymatic inactivation, diffusion and uptake
c. Release of trapping and scavenger molecules from the postsynaptic zone
d. Rise in synaptic pH and subsequent transmitter inactivation
e. Only by diffusion and uptake
b. Enzymatic inactivation, diffusion and uptake
A partial agonist will..
a. not influence the ratio of inactive to active state of the receptor
b. shift the ratio in favor of the active state
c. shift the ratio in favor of the inactive state
d. fix the ratio of inactive to active receptor at a given, agonist specific value, regardless of its concentration
d. fix the ratio of inactive to active receptor at a given, agonist specific value, regardless of its concentration
Beta-2-sympathomimetic drugs do not
a. Have an anabolic effect
b. Decrease heart rate
c. Used as tocolytics
d. Dilate arterioles
e. Cause bronchodilation
b. Decrease heart rate
