Please use this identifier to cite or link to this item:
https://hdl.handle.net/2440/5982
Citations | ||
Scopus | Web of ScienceĀ® | Altmetric |
---|---|---|
?
|
?
|
Type: | Journal article |
Title: | Comparative potencies of CGP 47654A and CGP 46165A as GABA (B) receptor antagonists in rat brain |
Author: | Ong, J. Kerr, D. Froestl, W. |
Citation: | European Journal of Pharmacology, 1999; 374(3):351-354 |
Publisher: | Elsevier BV |
Issue Date: | 1999 |
ISSN: | 0014-2999 1879-0712 |
Abstract: | In rat neocortical slices maintained in Mg2+-free Krebs medium, the gamma-aminobutyric acid (GABAB) receptor agonist baclofen concentration-dependently depressed the frequency of spontaneous discharges (EC50 = 6.1 microM). This was reversibly antagonised by 3-aminopropyl-(1,1-difluoro-n-butyl)-phosphinic acid (25, 100, 500 microM) (CGP 47654A) and 3-aminopropyl-P-(alpha-hydroxybenzyl)-phosphinic acid (CGP 46165A) (50, 100, 400 microM) which produced rightwards shifts of the baclofen concentration-response curves, with respective pA2 values of 4.9+/-0.2 and 4.6+/-0.15. Although relatively potent on GABAB heteroreceptors studied here, CGP 47654A and CGP 46165A were 5 and 50 times weaker, respectively, as GABAB autoreceptor antagonists [Froestl, W., Mickel, S.J., Von Sprecher, G., Diel, P.J., Hall, R.G., Maier, L., Strub, D., Melillo, V., Baumann, P.A., Bernasconi, R., Gentsch, C., Hauser, K., Jaekel, J., Karlsson, G., Klebs, K., Maitre, L., Marescaux, C., Pozza, M.F., Schmutz, M., Steinmann, M.W., Van Riezen, H., Vassout, A., Mondadori, C., Olpe, H.R., Waldmeier, P.C., Bittiger, H., 1995. Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists. J. Med. Chem. 38: 3313-3331.], representing potentially useful ligands for differentiating GABA hetero- and autoreceptors. |
Keywords: | Brain Neocortex Animals Rats Rats, Sprague-Dawley Phosphinic Acids Tritium gamma-Aminobutyric Acid Baclofen GABA Agonists Dose-Response Relationship, Drug Male GABA-B Receptor Antagonists In Vitro Techniques |
DOI: | 10.1016/S0014-2999(99)00377-5 |
Published version: | http://dx.doi.org/10.1016/s0014-2999(99)00377-5 |
Appears in Collections: | Anaesthesia and Intensive Care publications Aurora harvest 5 |
Files in This Item:
There are no files associated with this item.
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.