Molecular Pharmacology Exam 1

Questions.

Question 1.

Which of the following is not a cell surface target for drugs?

• a) Transporters
• b) Receptors
• c) Ion channels
• d) Carrier proteins

Question 2.

A drug with a pKb of 8 is in an environment of pH 7, what percentage of the drug would be ionized?

• a) 9%
• b) 91%
• c) 99%
• d) 1%

Question 3.

Below is the functional group on a tyrosine residue, what are the binding forces expected for this molecule?

• a) pi-cation
• b) Hydrogen bonding
• c) Ion -dipole
• d) ionic
• e) Hydrophobic

Question 4.

A drug inhibits AChE in the synaptic cleft of the neurons in a body. What effect would you not expect?

• a) Over signalling to mAChR
• b) Over signalling to nAChR
• c) A depletion in ACh production due to limited supply of Choline
• d) Over production of noradrenaline

Question 5.

Conformation restriction of a drug which mimics ACh can have a greater relative activity then ACh when acting in one receptor type. This is because:

• a) ACh is more optimized to fit into other receptor pockets
• b) ACh can take on more conformations in the active site
• c) The conformation restriction is binding allosterically, therefore, doesn’t need to fit in the pocket better
• d) The drug is simply bioisoteric, therefore, is less likely to be degraded

Question 6.

Which of the following is not a bioisoster of ACh

a)

b)

c)

d)

Question 7.

Which row of the table is correct

	Metabolized by AChE	Metabolized by BuChE	Metabolized by neither
a)	ACh	ACh	Carbachol
b)	ACh Benzylcholine Suxamethonium Butyryl Choline	Carbachol	ACh Methacholine
c)	ACh Methacholine	ACh Benzylcholine Suxamethonium Butyryl Choline	Carbachol
d)	AChE Methacholine	Benzylcholine Suxamethonium Butyryl Choline	Carbachol

Question 8.

Which of the following is not an AChE inhibitor

• a) Donepezil
• b) Physostigmine
• c) pralidoxime
• d) Organophosphates

Question 9.

Order the following interactions in chronological order for when a ACh interacts with AChE

• i. Movement down the active site gorge
• ii. Acetylation
• iii. Deacetylation
• iv. Attraction to the peripheral binding site

Question 10.

Which of the following is not a therapeutic use of AChE inhibitors

• a) Neostigmine enhancing nAChR activity for myasthenia gravis disease
• b) Physostigmine causing drainage of aqueous humour for glaucoma
• c) Pralidoxime regenerating phosphorylated AChE
• d) Donepezil increasing activity in basal forebrain for Alzheimer’s disease

Answers.

1. d) carrier proteins are intracellular targets
2. a)
3. d)
4. d)
5. b)
6. b)
7. c)
8. c)
   • a) Donepezil is non-competitive reversible AChE inhibitor, Physostigmine is a competitive reversible AChE inhibitor, Insecticides need to be metabolized first by insects, Organophosphates is irreversible AChE inhibitor. Paralidoxime
9. iv, i, ii, iii
10. c)