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Chronic administration of buspirone down‐regulates 5‐HT 2 receptor binding sites
Author(s) -
Taylor Duncan P.,
Hyslop Deborah K.
Publication year - 1991
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.430240108
Subject(s) - buspirone , pharmacology , anxiolytic , dopaminergic , serotonergic , antidepressant , chemistry , receptor , 5 ht receptor , autoreceptor , serotonin , endocrinology , medicine , dopamine , hippocampus
Buspirone (BuSpar®), a clinically effective anxiolytic, has been found in clinical trials to produce effects which suggest antidepressant efficacy. As antidepressants down‐regulate type 2 serotonin (5‐HT 2 ) receptors when given chronically to laboratory animals, we investigated whether buspirone would have similar effects; the possibility that chronic buspirone administration would affect β‐adrenergic, D‐2 dopaminergic, and γ‐aminobutyric acid (GABA) receptor binding was also investigated. When chronically administered in a regimen which reflected activity in an animal model of anxiety, buspirone produced significant decreases in in vitro 5‐HT 2 and β‐adrenergic receptor binding but was without effect on D‐2 dopaminergic of GABAergic binding. Ligand saturation experiments revealed that the decrease in 5‐HT 2 binding was due to a decrease in the maximal concentration of binding sites. These data demonstrate that chronic administration of buspirone to animals produces effects which suggest the potential for antidepressant efficacy in clinical use.