Raster, Peter and Spaeth, Andreas and Bultakova, Svetlana and Gorostiza, Pau and Koenig, Burkhard and Bregestovski, Piotr (2013) New GABA amides activating GABA(A)-receptors. BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY, 9. pp. 406-410. ISSN 1860-5397,
Full text not available from this repository. (Request a copy)Abstract
We have prepared a series of new and some literature-reported GABA-amides and determined their effect on the activation of GABA(A)-receptors expressed in CHO cells. Special attention was paid to the purification of the target compounds to remove even traces of GABA contaminations, which may arise from deprotection steps in the synthesis. GABA-amides were previously reported to be partial, full or superagonists. In our hands these compounds were not able to activate GABA(A)-receptor channels in whole-cell patch-clamp recordings. New GABA-amides, however, gave moderate activation responses with a clear structure-activity relationship suggesting some of these compounds as promising molecular tools for the functional analysis of GABA(A)-receptors.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | RECEPTOR FUNCTION; PHARMACOLOGY; SUBTYPES; GLUTAMATE; ABC; CHO-cells; GABA; GABA-amides; GABA-superagonist; patch-clamp recording |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institut für Organische Chemie > Lehrstuhl Prof. Dr. Burkhard König |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 28 Apr 2020 08:56 |
| Last Modified: | 28 Apr 2020 08:56 |
| URI: | https://pred.uni-regensburg.de/id/eprint/17134 |
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