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dc.contributor.authorOng, J.en
dc.contributor.authorMarino, V.en
dc.contributor.authorParker, D.en
dc.contributor.authorKerr, D.en
dc.contributor.authorFroestl, W.en
dc.identifier.citationEuropean Journal of Pharmacology, 1999; 383(2):137-141en
dc.description.abstractIn rat neocortical slices maintained in Mg(2+)-free Krebs medium, the gamma-aminobutyric acid (GABA(B)) receptor agonist baclofen concentration-dependently depressed the frequency of spontaneous discharges (EC(50)=12 microM). This was reversibly antagonised by (R, S)-3-amino-2-hydroxy-propyl-P-n-butyl-phosphinic acid (CGP 47332A) (25, 100, 300 microM) which produced rightwards shifts of the baclofen concentration-response curves (pA(2) value=4.8+/-0.1). In electrically stimulated slices preloaded with [3H]GABA, CGP 47332A increased its release (EC(150)=100 microM) through antagonism of GABA(B) autoreceptors. Although CGP 47332A was some six times weaker on GABA(B) auto- than on heteroreceptors, yet its congener lacking the beta-hydroxy substituent displays equal potency in both binding (IC(50)=38 microM) and GABA(B) autoreceptor functional studies (EC(150)=38 microM) as previously reported [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., Phosphinic acid analogues of GABA: 2. Selective, orally active GABA(B) antagonists. J. Med. Chem. 38 (1995) 3313-3331.].en
dc.rightsCopyright © 1999 Elsevier Science B.V. All rights reserved.en
dc.subjectGABAB receptor antagonist; Neocortical slices, rat; Baclofen; CGP 47332Aen
dc.titlePharmacological re-evaluation of a GABAB receptor antagonist CGP 47332A in rat brainen
dc.typeJournal articleen
pubs.library.collectionAnaesthesia and Intensive Care publicationsen
Appears in Collections:Anaesthesia and Intensive Care publications

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