1. G-protein coupled receptors are considered to be good drug targets because: A. their ligands will automatically be orally active B. the manner in which they interact with ligands is

1. G-protein coupled receptors are considered to be good drug targets because:
A. their ligands will automatically be orally active
B. the manner in which they interact with ligands is well understood
C. they are expressed in the nucleus
D. they generate second messenger molecules when activated
2. Over the last decade the trend in new drugs launched worldwide has been a:
A. fall in small organic molecules and biopharmaceuticals
B. fall in small organic molecules and growth in biopharmaceuticals
C. growth in small organic molecules and fall in biopharmaceuticals
D. growth in small organic molecules and in biopharmaceuticals
3. Development of a quantitative structure activity relationship (QSAR) requires
knowledge of the:
A. 3-dimensional structure of the drug
B. 3-dimensional structure of the drug target
C. physicochemical properties of the drug
D. physicochemical properties of the drug target
4. Gene arrays are used to compare the following in healthy and diseased tissues:
A. CDNA expression
B. genomic DNA expression
C. mRNA expression
D. protein expression patterns
5. Reverse pharmacology involves screening:
A. compound libraries against a novel receptor
B. natural products against a known receptor
C. orphan receptors for drug targets
D. the human genome for new drug targets 6. In relation to drug discovery, what does a reporter gene assay quantify?
A. Expression levels of a receptor protein
B. Gene expression in a tissue
C. Luciferase fluorescence in a receptor-expressing cell line
D. The activation of a receptor protein
7. In relation to drug receptor interactions, efficacy is the term used to describe the
capacity of an:
A. agonist to bind to a receptor
B. agonist to activate a receptor
C. antagonist to bind to a receptor
D. antagonist to inhibit a receptor
8. The shape of the theoretical curve that relates receptor occupancy to the log of
drug concentration is?
A. Hyperbolic
B. Linear
C. Log linear
D. Sigmoidal
9. A concentration-response curve for a drug may have a ll slope greater than
one due to:
A. drug metabolism
B. pharmacokinetic antagonism
C. positive cooperativety
D. the presence of multiple receptor subtypes Select the type of drug that best fits each of the following descriptions:
10. binds to receptors but does not stimulate the cell to respond
11. binds to receptors causing them to initiate a response, but unable to
evoke a maximal response even when occupying all receptors
12. binds to receptors, causes the cell to respond and is capable of eliciting
a maximal response
Options for 10-12:
A. antagonist
B. full agonist
C. inverse agonist
D. partial agonist
13. The potency of an antagonist is indicated by the following parameter:
A. efficacy
B. maximum response
C. PAZ
D. pD2
14. The following cannot be detected by a binding assay:
A. activation of G-protein coupled receptors
B. displacement of a radioligand from a receptor
C. ligand efficacy at a receptor
D. non-specific ligand binding
15. Which of the following tests would NOT employ a bioassay?
A. Identification of the effects of a new compound on cell secretion
B. Measurement of the activity of a new sample of insulin
C. Measurement of blood glucose levels
D. Measurement of the relative potency of two receptor agonists
16. Lead compounds will:
A. be completely non-toxic to cells
B. be detected in high-throughput screens
C. be freely soluble in water
D. have molecular weights greater than 600 17. Mix and split synthesis is a type of:
A. combinational chemistry
B. combinatorial chemistry
C. computational chemistry
D. computerised chemistry
18. In relation to drug discovery an "Active" is a compound that has an effect in a
biological screen:
A. and can be optimised to produce a lead
B. and is active in vivo
C. but may not bind to the target
D. by binding to the target
19. In optimising a lead molecule, the goal is to produce a compound with properties
that include:
A. can be made into a tablet for oral administration
B. efficacy = 1
C. high potency against the molecular target
D. not metabolised in vivo
For questions 20 and 21
100
The figure to the left plots contractile
responses of guinea-pig isolated ileum at
increasing concentrations of three drugs
(A, B and C) acting at the same receptor.
Response (% of maximum)
50
Use this information to answer questions
20 and 21.
0.01
0.1
1.0
10
100
Acetylcholine concentration, JIM (log scale) 20. The ECso of drug B is:
A. 10*M
B. 10"M
C. 10* M
D. 10’M
21. is the order of drug potency (lowest to highest)?
A. A < B< C
B. B <C<A
C. C <B <A
D. C =B <A
For questions 22-30 choose the ONE INCORRECT response from the options provided
22. A scintillation proximity assay:
A. detects the release of B particles
B. employs scintillant-containing microbeads
C. employs microbeads with an attached receptor
D. requires separation of bound and free ligand
23. gh-throughput screening:
A. can be used to screen hundreds of thousands of compounds in a week
B, can give reliable indications of in vivo activity
C. is dependent upon robotic technology
D. relies upon the precise identification of the drug target
24. Lipinski’s "Rule of Five" requires that drug candidates:
A. contain no more than 5 hydrogen bond donors
B. contain no more than 10 hydrogen bond acceptors
C. have a molecular mass more than 500 daltons
D. have log P less than 5 25. Capillary endothelial cells of the blood brain barrier:
A. are connected by tight junctions
B. contain P-glycoprotein, which s drug molecules to cross into brain tissue
C. contain phospholipids that to repel some drugs
D. prevent as much as 98% of potentially beneficial drugs from reaching the brain
26. Excipients in a tablet could include:
A. a buffering agent
B. a colouring agent
C. a lubricant
D. an active drug
27. The core battery of pharmacology studies that are required to demonstrate the
safety of a drug for use in man include studies on the:
A. cardiovascular system
B. central nervous system
C. genito-urinary system
D. respiratory system
28. Methods for studying the metabolism of drugs make use of:
A. computer algorithms to predict the stability of molecular structures
B. hepatocytes isolated from liver
C. microsomes prepared from liver hepatocytes
D. S9 cell fractions containing the cytosol and nucleus
29. Phase II metabolic reactions generally result in drug molecules:
A. becoming more water soluble
B. being less pharmacologically active
C. being more easily excreted
D. having a smaller molecular weight
30. Pharmacodynamic biomarkers indicate:
A. how a drug is metabolised
B. if a drug has interacted with a target
C. if a drug has modulated a target
D. the efficacy of a drug candidate

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