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[ 3 H]Citalopram Binding to Brain and Platelet Membranes of Human and Rat
Author(s) -
Plenge Per,
Mellerup Erling T.
Publication year - 1991
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1991.tb02588.x
Subject(s) - citalopram , membrane , platelet , chemistry , neuroscience , biophysics , medicine , serotonin , biochemistry , biology , receptor
Citalopram, a selective serotonin (5‐HT) uptake inhibitor with antidepressant properties, was found to bind with high affinity to the 5‐HT transporter from human neuronal and platelet membranes. At 20°C, K D was about 1.5 n M in both tissues. [ 3 H]Citalopram bound to rat neuronal membranes with higher affinity than to human neuronal and platelet membranes; at 20°C K D was about 0.7 n M . The B max value for the binding of [ 3 H]citalopram to platelet membranes was close to that found using the 5‐HT uptake inhibitors [ 3 H]imipramine and [ 3 H]paroxetine, suggesting that all three 5‐HT uptake inhibitors bind to the 5‐HT transporter. The dissociation rate of [ 3 H]citalopram increased twofold with each 4–5°C increase in temperature in both human and rat membranes, although at any given temperature, the dissociation rate was about four times faster in the human neuronal and platelet membranes than in rat neuronal membranes.