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The aim of this chapter is to consider the structure, distribution and functional properties of neurotransmitter receptors in the brain in general and discuss the principles of how the action of drugs at these receptors can be studied. Diversity of neurotransmitter action is provided by the presence of multiple receptor subtypes for each neurotransmitter, all of which still remain specific to that neurotransmitter. This principle is illustrated by the simple observations outlined in Neurotransmitters, Drugs and Brain Function. These simple qualitative observations by Langley and others at the beginning of the twentieth century led to the development of more quantitative pharmacological methods that were subsequently used to identify and classify receptors. On the other hand, if, as Ahlquist first found in the s, these compounds give a distinct order of potency in some of the tests, but the reverse or just a different order in others, then there must be more than one type of receptor for these agonists. In fact, careful quantitative analysis of the order of activity of the agonists in each test, and of the precise potency of antagonists see Chapter 5 for quantitative detail has often successfully indicated, although rarely proved, the presence of subclasses of a receptor type e.

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