[3H]5-hydroxytryptamine binding sites in postmortem human brain.
Binding sites for [3H]5-hydroxytryptamine (5-HT) in postmortem human frontal cortex, hippocampus and amygdala were studied by displacement with 5-HT selective drugs. The results demonstrated the selective labelling of 5-HT1-like sites by [3H]5-HT in the cortex, with little or no labelling of 5-HT2 or 5-HT3 sites. Self-displacement of the binding of [3H]5-HT is consistent with the presence of a single population of sites, indicating that 5-HT is non-selective for the 5-HT1 subtypes. Around 40% of the 5-HT1 sites in the frontal cortex and amygdala were of the 5-HT1A subtype, in contrast to 60% in the hippocampus. The drug RU 24969 consistently displaced with, a high affinity, a greater proportion of [3H]5-HT sites than did 8-OH-DPAT in all three regions of the brain. The nature of these additional sites was not established. A small proportion (less than 10%) of [3H]5-HT sites in the frontal cortex appeared to be of the 5-HT1C subtype, as these sites were displaced with high affinity by mianserin.
Cheetham
S C
SC
Department of Pharmacology and Clinical Pharmacology, St George's Hospital Medical School, London, U.K.
Yamaguchi
Y
Y
Horton
R W
RW
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D000679:Amygdala / Q000187:drug effects / Q000378:metabolism; D001667:Binding, Competitive / Q000187:drug effects; D001923:Brain Chemistry; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology; D007700:Kinetics; D008297:Male; D008566:Membranes / Q000378:metabolism; D008875:Middle Aged; D011180:Postmortem Changes; D011985:Receptors, Serotonin / Q000378:metabolism*; D013764:Tetrahydronaphthalenes / Q000494:pharmacology
D007211:Indoles; D011985:Receptors, Serotonin; D013764:Tetrahydronaphthalenes; C025145:5-methoxy 3-(1,2,3,6-tetrahydro-4-pyridinyl)1H indole; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin