Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3 Suppl
pubmed:dateCreated
1990-9-5
pubmed:abstractText
Preclinical neurochemical studies indicate that buspirone and gepirone bind selectively to presynaptic (dorsal raphe) and postsynaptic (hippocampus, cortex) 5-hydroxytryptamine1A (5-HT1A) receptor binding sites. Furthermore, in functional neurochemical and electrophysiologic receptor studies, azapirones in general display partial agonist activity at postsynaptic 5-HT1A receptors linked negatively to adenyl cyclase and appear to demonstrate a similar profile on hippocampal CA1 pyramidal neurons sensitive to the effects of 5-HT. Through their action at presynaptic 5-HT1A receptors, these agents have been shown to dose-dependently inhibit cortical and hippocampal 5-HT synthesis while inhibiting the firing of 5-HT--containing dorsal raphe neurons, both in vitro and in vivo. These results suggest that the efficacy seen in clinical trials of anxiety and depression may be related to buspirone's and gepirone's complex interaction with presynaptic and postsynaptic 5-HT1A receptors, which initiate long-term changes in central 5-HT neurotransmission.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0271-0749
pubmed:author
pubmed:issnType
Print
pubmed:volume
10
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
6S-12S
pubmed:dateRevised
2005-11-16
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Neurochemistry and neurophysiology of buspirone and gepirone: interactions at presynaptic and postsynaptic 5-HT1A receptors.
pubmed:affiliation
CNS Pharmacology, Bristol-Myers Squibb Company, Wallingford, CT 06492-7660.
pubmed:publicationType
Journal Article, Review