Medicinal Chemistry

c. M—Metabolism competition (competition for same enzymes in liver).

d. E—Elimination competition (similar structures are competitive for kidney

excretion).

3. Pharmaceutical drug–drug interactions
   Chemical reaction in gut (e.g., co-administration of valproic acid with an antacid).


4. Adjunctive polypharmacy
   Two different drugs targeting completely different aspects of a common disease
   (e.g., giving an antiplatelet agent and an antihypertensive agent to a person with
   a stroke; one agent treats platelet clots that may cause stroke, the other agent treats
   the high blood pressure that also may cause strokes).

Selected References

General References on Receptors

D. R. Burt (1985). Criteria for receptor identification. In: H. T. Yamamura, S. J. Enna, M. J. Kuhar
(Eds.).Neurotransmitter Receptor Binding,2nd ed. New York: Raven Press, pp. 41–60.
P. Ehrlich (1897). Klin Jahr. 6: 299.
R. Flower (2002). Drug receptors: a long engagement. Nature 415: 587.
B. G. Katzung (Ed.) (2001). Basic and Clinical Pharmacology, 8th ed. New York: Lange.
A. Korolkovas (1970). Essentials of Molecular Pharmacology. New York: John Wiley.
J. Langley (1878). J. Physiol. (London) 1 : 367.
H. Lullmann, K. Mohr, A Ziegler, D. Bieger (2000).Color Atlas of Pharmacology. New York: Thieme.
J. Parascandola (1980). Origins of the receptor theory. Trends Pharmacol. Sci. 1 : 189–192.
D. F. Smith. (Ed.) (1989).CRC Handbook of Stereoisomers: Therapeutic Drugs. Boca Raton:
CRC Press.

Drug–Receptor Interaction Forces

P. Andrews (1986). Functional groups, drug–receptor interactions and drug design. Trends
Pharmacol. Sci. 7: 148–151.
A. Ben-Nairn (1980).Hydrophobic Interactions. New York: Plenum.
P. H. Doukas (1975). The role of charge-transfer processes in the action of bioactive materials.
In: E. J. Ariëns (Ed.).Drug Design, vol. 5. New York: Academic Press, pp. 133–167.
P. A. Kollman (1980). The nature of the drug–receptor bond. In: M. F. Wolff (Ed.). The Basis of
Medicinal Chemistry,4th ed. Part 1. New York: Wiley-Interscience, pp. 313–329.
J. B. Stenlake (1979).Foundations of Molecular Pharmacology,vol. 2. London: Athlone Press,
chapter 2.

Quantifying Receptor Binding

A. De Lean, D. Rodbard (1979). Kinetics of cooperative binding. In: R. D. O’Brien (Ed.). The
Receptors. New York: Plenum Press, pp. 140–192.
D. G. Haylett (2003). Direct measurement of drug binding to receptors. In:Textbook of Receptor
Pharmacology, 2nd ed. Boca Raton: CRC Press, pp. 153–180.
J. M. Klotz, D. L. Hunston (1971). Properties of graphical representation of multiple classes of
binding sites. Biochemistry 10: 3065–3069.

RECEPTORS: STRUCTURE AND PROPERTIES 103