Back to Search
Start Over
Short-chain baclofen analogues are GABAB receptor antagonists in the guinea-pig isolated ileum.
- Source :
-
European journal of pharmacology [Eur J Pharmacol] 1991 Dec 03; Vol. 205 (3), pp. 319-22. - Publication Year :
- 1991
-
Abstract
- A new series of GABAB receptor antagonists, based on short-chain baclofen analogues has been investigated. In guinea-pig isolated ileal preparations, the GABAB receptor-mediated, baclofen-induced depression of cholinergic twitch responses was reversibly and competitively antagonised by the short-chain baclofen analogues 3-amino-3-(p-chlorophenyl)propionic acid (apparent pA2 = 3.5), 2-amino-2-(p-chlorophenyl)ethanephosphonic acid (apparent pA2 = 3.8), and 2-amino-2-(p-chlorophenyl)ethanesulphonic acid apparent pA2 = 4.0). The corresponding des-chloro analogues were all less active. These compounds represent another class of GABAB receptor antagonists which may cross the blood-brain barrier.
- Subjects :
- Aminoethylphosphonic Acid analogs & derivatives
Animals
Baclofen antagonists & inhibitors
Baclofen pharmacology
Female
Guinea Pigs
Ileum drug effects
Ileum physiology
Ileum ultrastructure
In Vitro Techniques
Male
Muscle Contraction drug effects
Muscle, Smooth physiology
Muscle, Smooth ultrastructure
Phenylalanine analogs & derivatives
Phenylalanine pharmacology
Taurine analogs & derivatives
beta-Alanine analogs & derivatives
Baclofen analogs & derivatives
GABA-A Receptor Antagonists
Muscle, Smooth drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0014-2999
- Volume :
- 205
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- European journal of pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 1667917
- Full Text :
- https://doi.org/10.1016/0014-2999(91)90918-g