Binding of the novel serotonin agonist 8-hydroxy-2-(di-n-propylamino) tetralin in normal and Alzheimer brain.
Binding of [3H]8-hydroxy-2-(di-n-propylamino) tetralin, a putative ligand for the 5-hydroxytryptamine (5-HT, serotonin) 1A recognition site, was measured in neocortex from postmortem human brain. The substance was found to bind to a saturable site with a KD value and pharmacological profile similar to that of rat. Binding to membranes from normal human temporal cortex was found to significantly correlate (inversely) with age. A significant reduction in binding, reflecting decreased density of recognition sites, was observed in the frontal cortex of patients with Alzheimer's disease (48% loss). This region in the dement brains showed unaltered presynaptic 5-HT function (5-HT and 5-hydroxyindoleacetic acid content) whereas 5-HT concentration was reduced in the temporal cortex.
Middlemiss
D N
DN
Palmer
A M
AM
Edel
N
N
Bowen
D M
DM
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000544:Alzheimer Disease / Q000378:metabolism*; D001665:Binding Sites; D001921:Brain / Q000378:metabolism*; D002540:Cerebral Cortex / Q000378:metabolism; D005625:Frontal Lobe / Q000378:metabolism; D006897:Hydroxyindoleacetic Acid / Q000378:metabolism; D009281:Naphthalenes / Q000378:metabolism*; D012701:Serotonin / Q000378:metabolism; D013702:Temporal Lobe / Q000378:metabolism; D013764:Tetrahydronaphthalenes / Q000378:metabolism*
D009281:Naphthalenes; D013764:Tetrahydronaphthalenes; D012701:Serotonin; D006897:Hydroxyindoleacetic Acid; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin