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3-amino-2-(4-chlorophenyl)-nitropropane is a new GABAB receptor agonist, more active peripherally.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1993 May 19; Vol. 236 (2), pp. 239-45. - Publication Year :
- 1993
-
Abstract
- The activity of the nitropropane analog of baclofen, 3-amino-2-(4-chlorophenyl)-nitropropane (N-BAC), has been examined at central and peripheral GABAB receptors. N-BAC was less potent than baclofen as a GABAB receptor agonist in depressing repetitive twitch contractions in the guinea-pig isolated ileum (IC50s for baclofen = 4.1 +/- 1.3 microM; N-BAC = 9.2 +/- 0.3 microM) and vas deferens (IC50s for baclofen = 30 microM; N-BAC = 100 microM), competitively antagonised by phaclofen, 2-hydroxysaclofen and CGP 35348 (3-aminopropyl-P-di-ethoxymethylphosphinic acid). In the ileum, the pA2 values for CGP 35348 with baclofen (4.7 +/- 0.2) and N-BAC (4.6 +/- 0.3) were not significantly different (P > 0.05), indicating that both agonists activate the same receptor type. By contrast, in rat neocortical slices, N-BAC was 20 times weaker than baclofen in attenuating spontaneous discharges, sensitive to CGP 35348, whilst it was 100 times less potent than baclofen in depressing evoked CA1 population spikes in the hippocampus. This new GABAB receptor agonist, N-BAC, is thus more active at peripheral than central GABAB receptors.
- Subjects :
- Animals
Baclofen analogs & derivatives
Baclofen antagonists & inhibitors
GABA-A Receptor Antagonists
Guinea Pigs
Male
Muscle, Smooth drug effects
Nitro Compounds antagonists & inhibitors
Organophosphorus Compounds pharmacology
Propylamines antagonists & inhibitors
Rats
Rats, Sprague-Dawley
Vas Deferens drug effects
Baclofen pharmacology
Brain drug effects
Muscle Contraction drug effects
Nitro Compounds pharmacology
Propylamines pharmacology
Receptors, GABA-A drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 236
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 8391459
- Full Text :
- https://doi.org/10.1016/0014-2999(93)90594-8