Inhibition of MAO activity, 3H-imipramine binding, 3H-paroxetine binding and 3H-5-HT uptake by human cerebrospinal fluid.
Addition of small amount of human cerebrospinal fluid (CSF) inhibited both types of MAO in monkey brain mitochondria. The specific binding of 3H-paroxetine decreased remarkably with increasing CSF volumes, while 3H-imipramine binding was slightly inhibited. Scatchard analysis of 3H-paroxetine binding in the presence and absence of CSF indicated that the inhibitory effect was associated with a decreased Bmax without an appreciable change in Kd. Addition of CSF induced an inhibition of uncompetitive 3H-5-HT uptake to monkey cerebral membranes. These results indicate that the materials in human CSF inhibit 3H-paroxetine binding, and modulate the uptake system for 5-HT.
Egashira
T
T
Department of Pharmacology, Medical College of Oita, Japan.
Goto
S
S
Murayama
F
F
Yamanaka
Y
Y
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism / Q000648:ultrastructure; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D002555:Cerebrospinal Fluid / Q000502:physiology*; D006801:Humans; D007099:Imipramine / Q000378:metabolism*; D007700:Kinetics; D008253:Macaca mulatta; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D008928:Mitochondria / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors; D017374:Paroxetine; D010880:Piperidines / Q000378:metabolism*; D011955:Receptors, Drug / Q000187:drug effects; D012701:Serotonin / Q000378:metabolism*
D008996:Monoamine Oxidase Inhibitors; D010880:Piperidines; D011955:Receptors, Drug; D012701:Serotonin; D017374:Paroxetine; D007099:Imipramine