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Concepts for the design of 5‐HT 1A serotonin agonists and antagonists
Author(s) -
Glen Richard A.
Publication year - 1992
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430260306
Subject(s) - serotonergic , agonist , antagonist , partial agonist , postsynaptic potential , serotonin , pharmacology , chemistry , neuroscience , psychology , medicine , receptor , biochemistry
The accessibility and use of a standard 5‐HT 1A agonist radioligand ([ 3 H]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‐HT 1A 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‐HT 1A serotonergic agents and the available data on their 5‐HT 1A agonist and antagonist activity with the aim of formulating SAR. These SAR should provide useful information for the subsequent design of 5‐HT 1A ‐selective agonists and antagonists. © 1992 Wiley‐Liss, Inc.