Concepts for the design of 5‐HT1A serotonin agonists and antagonists

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Abstract
The accessibility and use of a standard 5‐HT1A agonist radioligand ([3H]8‐hydroxy‐2‐(dipropylaminotetralin) has resulted in the availability of a large amount of binding data on various serotonergic agents. This, in turn, has permitted the formulation of structure—affinity relationships (SAFIR). By contrast, much less information is available concerning the agonist and antagonist activity of these agents. This is primarily due to a lack of standard evaluation procedures, controversy regarding the presynaptic versus postsynaptic nature of certain models, and the recent realization that many 5‐HT1A agents are partial agonists. Thus, it has been difficult to formulate structure—activity relationships (SAR) for these agents. The present review examines the various classes of 5‐HT1A serotonergic agents and the available data on their 5‐HT1A agonist and antagonist activity with the aim of formulating SAR. These SAR should provide useful information for the subsequent design of 5‐HT1A‐selective agonists and antagonists.