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.
- d) carrier proteins are intracellular targets
- a)
- d)
- d)
- b)
- b)
- c)
- 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
- iv, i, ii, iii
- c)