Reference no: EM133228963

1. State some factors that influence the bioavailability of a drug molecule following oral absorption. 

2. Draw and explain the Newman projections of acetylcholine.

3. Explain how polycyclic structures, such as decaline or the steroids, are rigid and maintain stable conformations. 

4. Explain what role does aromatic rings play in drug design. 

5. Explain the steric Effects on Drug-Receptor Interactions.

6. Explain what is a Taft steric parameter. 

7. The difference in pharmacological action between enantiomers can be considerable. Explain this using (-)-Levorphanol and (+)-Dextrorphan. 

8. Explain what is a eudismic ratio. 

9. Explain some unwanted effects of a distomer. 

10. Explain what is meant electronic properties of drug molecules. 

11. Explain the difference between Direct electronic effects Indirect electronic effects during drug-receptor interactions. 

12. Explain how the Hammet Correlations has been used to quantify Drug Molecule Electronic Properties. 

13. Explain why the pKa of a drug is important to its pharmacological activity. 

14. Explain how the electron distribution in a drug molecule can be estimated or determined by experiment. 

15. Explain the role of molecular quantum mechanics calculations involved in drug molecules. 

16. Write the Schrödinger equation. Explain why in quantum pharmacology, the goal is to determine the wavefunction. 

17. Explain the difference between molecular mechanics (MM) and quantum mechanics (QM). Elaborate on the strengths and weaknesses of QM and MM. 

18. Outline the strengths and weaknesses of experimental techniques such as NMR and X-ray crystallography against theoretical techniques such as quantum mechanics and molecular mechanics when determining the structure of drug molecules.  

19. Describe some classes of drug receptor molecules. 

20. It is important to use an extensive set of criteria for receptor identification in both in vitro and in vivo studies. Explain these criteria. 

21. Since the association of small molecules (e.g., drugs) with macromolecules (e.g. receptors) is promoted and stabilized by intermolecular interactions, an understanding of the nature of chemical bonds and intermolecular interactions is of great interest to the medicinal chemist. Explain the various types of intermolecular interactions and their average energies. 

22. Explain how penicillin attaches to a receptor. 

23. When designing a drug, the designer wishes to have an energetically favorable and geometrically optimal interaction with the receptor site. Explain how these are achieved. 

24. Explain the functional Molecular Properties of Drug Receptors. 

25. Explain the Molecular-Level Conceptual Models of Receptors 

26. Make brief notes on the following: 

• Receptor Regulation at the Genetic Level
• Receptor Regulation by Ligand
• Covalent Modification of Receptors
• Noncovalent Modification of Receptors
• Receptor Clustering
• Receptor Internalization 

27. Explain the following: 

(i) The Adenylate Cyclase System 

(ii) The Guanylate Cyclase System

(iii) The Inositol Triphosphate-Diacylglycerol System 

28. Discuss the 3 basic approaches to receptor site selection.