General Principles Of Pharmacology/Sites of Drug Action
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The major sites of action for drugs are receptors. This section reviews important concepts related to drug-receptor
interactions.
The first discussions of the concept of a receptor were presented by J.N. Langley (1878), studying the action of atropine and pilocarpine on salivary flow in cats. Langley referred to the receptive substance of muscle that received the stimulus and transferred it to the contractile material. The term receptor, however, was first used by P. Ehrlich (1913) to describe hypothetical specific chemical groupings of "side chains" on cells upon which chemotherapeutic agents were postulated to act.
Normal Physiology
Most forms of communication between cells are mediated by receptor-ligand interactions. For example, the movement of skeletal muscles is entirely dependent upon the interaction of acetylcholine with the acetylcholine receptor at the neuromuscular junction. The control of heart rate is mediated by central nervous system neurotransmitter receptors and receptors in the autonomic nervous system. In addition, all hormone action is mediated by either membrane bound receptors on the cell surface or soluble receptors in the cytoplasm.
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