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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
Issue Date: 1999
ISSN: 0014-2999
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
RMID: 0030006086
DOI: 10.1016/S0014-2999(99)00377-5
Appears in Collections:Anaesthesia and Intensive Care publications

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