The occupancy theory receptor theory drug action

This examination booklet consists of 20 pages, numbered 1-20 inclusive. There are 43 questions, numbered 1- 43 inclusive. Students are asked to check that their booklet is complete, and to indicate that they have done so by signing below.

Q6.	Semester 1 – June, 2014			Page 3 of 20
	Which of the following criteria is the most important to be met for a drug to be considered a lead compound:


	E.	understanding of the biochemistry of the disease state optimising the pharmacokinetic and pharmacodynamic properties of drug candidates evaluation of the screened compounds.

		the maximum strength of the effect of the drug . the amount of drug required for a specific effect to occur.

A. B. C. D. E.	answers B and C are correct.

Q11. The occupancy theory of receptor theory of drug action:

	the maximum amount of binding. the measurement of free and bound ligand concentrations. the equilibrium dissociation constant.

Q13. The characteristics of a standard combinatorial chemistry library are

A. B. C. D. E.

	Labile under most reaction conditions. Reacts slowly with starting material.

Q16. The following is an important resin used in combinatorial chemistry.

O	NH2

	Purifying a lead compound. Optimising a lead compound.

*** ROUGH WORK SPACE ***

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	Semester 1 – June, 2014	Page 9 of 20

Q23. Which of the following statements are CORRECT?

Q24. Gs

	Semester 1 – June, 2014	Page 10 of 20

Q26. LogP:

	is equal to the log of the octanol-water partition coefficient of a pure compound is equal to the log of the sum of the π values.

Q27. Comparative Molecular Field Analysis (CoMFA) and Comparative Molecular Similarity Indices (CoMSIA):

Q29. Which one of the following Michaelis-Menten plots represents active site noncompetitive

reversible enzyme inhibition?

D. Plot 4

E. None of the above

Q31. Enzymes catalyse reactions by:

A. B. C. D. E.

A. B. C. D. E.	inhibitory ligand gated ion channels exitatory ligand gated ion channels G-protein coupled receptors that mediate their effect through Gi/o G-protein coupled receptors that signal through Gq/11 linked to different G-proteins depending on which cell they are located in

9184	Semester 1 – June, 2014	Page 13 of 20

(6 marks)

A. What are these specific stages?

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Q40. Outline a common procedure for assessment of the predictive power of a QSAR model. (4 marks)

Q41. The kinetics of the enzyme E as a function of substrate concentration is presented using

A. Find Vmax (apparent) of inhibitor A. (2 marks)

	Semester 1 – June, 2014	Page 20 of 20

X-Ray Crystallography	Homology Modeling

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