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DOI: 10.1055/s-2000-11112
Evidence for Specific Interactions between Kavain and Human Cortical Neurons Monitored by Fluorescence Correlation Spectroscopy
Publication History
Publication Date:
31 December 2000 (online)
Abstract
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 μM 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.
Key words
Kavain, kavapyrones - Piper methysticum - Piperaceae - fluorescence correlation spectroscopy
References
- 1 Kretzschmar R,, Meyer H J,, Teschendorf H J.. . Experientia. 1970;; 26 283-284
- 2 Kretzschmar R,, Meyer H J.. . Arch. Int. Pharmacodyn.. 1969;; 180 475-491
- 3 Ferger B,, Boonen G,, Häberlein H,, Kuschinsky K.. . Eur. J. Pharmacol.. 1998;; 347 211-214
- 4 Gleitz J,, Beile A,, Peters T.. . J. Neuropharmac.. 1995;; 9 113-138
- 5 Gleitz J,, Beile A,, Peters T.. . J. Neuropharmac.. 1996;; 35 179-186
- 6b Magura E I,, Kopanitsa M V,, Gleitz J,, Peters T,, Krishtal O A.. . Neuroscience . 1997;; 81 345-351
- 6a Hänsel R,. . Pacific Sci.. 1968;; 22 293-313
- 7 Backhauß C,, Krieglstein J.. . Eur. J. Pharmacol.. 1992;; 215 265-269
- 8 Davies L,, Colleen A D,, Duffield P,, Johnston G AR,, Jamieson D D.. . Pharmac. Toxic.. 1992;; 71 120-126
- 9 Jussofie A,, Schmiz A,, Hiemke C.. . Psychopharmacology. 1994;; 116 469-474
- 10 Boonen G,, Häberlein H.. . Planta Med.. 1998;; 64 504-506
- 11 Rigler R.. . J. Biotech.. 1995;; 41 177-186
- 12 Rauer B,, Neumann E,, Widengren J,, Rigler R.. . Biophys. Chem.. 1996;; 58 3-12
- 13 Rigler R,, Mets Ü,, Widengren J,, Kask P.. . Eur. Biophys. J.. 1993;; 22 169-175
- 14 Marquardt D W.. . J. Soc. Indust. Appl. Math.. 1963;; 11 431-441
- 15 Häberlein H,, Boonen G,, Beck M-A.. . Planta Med.. 1996;; 63 63-65
- 16 Ehrenberg M,, Rigler R.. . Chem. Phys.. 1974;; 4 390-401
- 17 Elson E L,, Magde D.. . Biopolymers. 1974;; 13 1-27
- 18 Koppel D.. . Physical Rev.. 1974;; A10 1938-1945
- 19 Eigen M,, Rigler R.. . Proc. Natl. Acad. Sci. USA. 1994;; 91 5740-5747
- 20 Rigler R,, Mets Ü.. . Soc. Photo-Opt. Instrum. Engrs.. 1992;; 1921 239-248
- 21 Rigler R,, Widengren J.. . Bioscience. 1990;; 3 180-183
Dr. Hanns Häberlein
Institut für Pharmazeutische Biologie
Philipps-Universität Marburg
Deutschhausstraße 17A
D-35032 Marburg
Germany
Email: haeberlh@mailer.uni-marburg.de
Phone: +49-6421-2825369