Evidence for specific interactions between kavain and human cortical neurons monitored by fluorescence correlation spectroscopy.
Specific interactions between a tetramethylrhodamine-labeled kavain derivative and human cortical neurons were found for the first time using fluorescence correlation spectroscopy (FCS). Human cortical neurons, cultivated in Nunc chambers, were incubated with 1 nM of the dye-labeled kavain derivative. A total binding of 0.55 nM was found after an incubation period of 60 min. 50% of the total binding was specifically displaced in the presence of 1 microM non-labeled (+)-kavain. Evidence for these specific interactions was verified by a saturation experiment. Both the non-linear Scatchard plot and the n value of 1.58 +/- 0.07 in the sigmoid Hill plot indicate binding sites with different binding affinities.
Boonen
G
G
Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden.
Pramanik
A
A
Rigler
R
R
Häberlein
H
H
D002478:Cells, Cultured; D002540:Cerebral Cortex / Q000166:cytology / Q000187:drug effects*; D006801:Humans; D009474:Neurons / Q000187:drug effects*; D011753:Pyrones / Q000494:pharmacology*; D013050:Spectrometry, Fluorescence
D011753:Pyrones; C011889:kavain