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Antagonism at GABAB receptors by saclofen and related sulphonic analogues of baclofen and GABA.
- Source :
-
Neuroscience letters [Neurosci Lett] 1989 Dec 15; Vol. 107 (1-3), pp. 239-44. - Publication Year :
- 1989
-
Abstract
- Saclofen (the direct sulphonic analogue of baclofen) is a competitive antagonist of baclofen at GABAB receptors in guinea pig ileum and rat cortical slices (estimated pA2 = 5.3), at least twice as potent as 2-hydroxy-saclofen (pA2 = 5). A series of related sulphonic analogues also antagonised baclofen in the guinea pig ileum, including 2-hydroxy-saclofen amide (pA2 = 3.3), 3-amino-2-hydroxy-2-phenyl-propylsulphonic acid (pA2 = 3.5), 3-amino-2-(benzo-(b)-furan-2-yl)-propylsulphonic acid (pA2 = 4.3), and 3-amino-2-(4-chlorophenyl)-prop-1-enesulphonic acid (pA2 = 2.5-3), but none were more active than saclofen which is the most potent specific GABAB antagonist yet found.
- Subjects :
- Animals
Cerebral Cortex drug effects
Evoked Potentials drug effects
GABA-A Receptor Antagonists
Guinea Pigs
Ileum drug effects
Ileum physiology
Muscle, Smooth drug effects
Baclofen analogs & derivatives
Baclofen pharmacology
Cerebral Cortex physiology
Ileum innervation
Muscle Contraction drug effects
Muscle, Smooth innervation
Receptors, GABA-A physiology
gamma-Aminobutyric Acid pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0304-3940
- Volume :
- 107
- Issue :
- 1-3
- Database :
- MEDLINE
- Journal :
- Neuroscience letters
- Publication Type :
- Academic Journal
- Accession number :
- 2559370
- Full Text :
- https://doi.org/10.1016/0304-3940(89)90824-0