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The 5-hydroxytryptamine 5-HT1A receptor has been the focus of considerable research effort for over a decade. However, the definitive classification of this receptor and the full characterization of its pharmacology have awaited the development of highly selective 5-HT1A receptor antagonists. The only compounds available until recently have been either nonselective or partial 5-HT1A receptor agonists (or a combination of both). Confusion has arisen owing to the use of different pharmacological models in examining the functional activity of 5-HT1A receptor ligands. Several partial agonists display only antagonist activity in models of postsynaptic 5-HT1A receptor function, whereas their agonist properties are revealed in models of presynaptic, somatodendritic 5-HT1A autoreceptor function. In view of these considerations, the term 'silent antagonist' has been introduced to distinguish true 5-HT1A receptor antagonists from partial agonists. Allan Fletcher and colleagues review the pharmacological properties of the first selective silent 5-HT1A receptor antagonists that have been recently discovered and discuss the potential therapeutic utility of these novel compounds.

Type

Journal article

Journal

Trends Pharmacol Sci

Publication Date

12/1993

Volume

14

Pages

41 - 48

Keywords

Animals, Binding Sites, Hippocampus, Humans, Mental Disorders, Rats, Receptors, Serotonin, Serotonin Antagonists, Serotonin Receptor Agonists