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General Principles Of Pharmacology/Molecular aspects of binding

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Previous Page: Binding and Response

The forces that determine whether or not a drug will interact with a receptor are thermodynamic and include enthalpy (the absorption or production of heat) and entropy (the increase or decrease in disorder). Production of heat (a decrease in enthalpy) and/or an increase in disorder (an increase in entropy) are associated with the formation of a chemical bond between the receptor and drug. The types of chemical bonds that can be formed between a receptor and drug are:

•Covalent: This is the strongest chemical bond and is usually associated with a drug that interacts irreversibly with a receptor. Most drugs do not form covalent bonds.

•Electrostatic: This is a very common type of bond between a receptor and drug. It is due to the attraction between oppositely charged groups on the receptor and drug. Electrostatic interactions include a simple attraction between positive and negative charges and more complex interactions between polar groups.

•Hydrogen: A hydrogen bond represents a strong interaction between a drug and receptor and arises from the sharing of a hydrogen atom between an acidic group and a basic group.

• van der Waals: A weak attraction between either polar or nonpolar molecules. It is essentially electrostatic in nature and varies with distance.

• Hydrophobic: This can be a major driving force for a binding interaction if the drug and/or binding site is nonpolar. The basis of this effect is that the interaction of nonpolar surfaces with water is unfavorable and that by removing two nonpolar surfaces from an interaction with water, a net attractive force is produced.

Next Page: Measurement of Effect
Previous Page: Binding and Response

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