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Characterization of GABAB ligands in vivo.
- Source :
-
General pharmacology [Gen Pharmacol] 1995 Mar; Vol. 26 (2), pp. 417-24. - Publication Year :
- 1995
-
Abstract
- 1. While GABAB antagonists have been examined in vitro, very few have been tested in vivo. A range of GABAB antagonists were tested against baclofen-induced muscle relaxation and hypothermia. 2. The GABAB antagonists exhibited a range of in vivo activity profiles. 3. CGP 35348 showed clear antagonist effects, while BPBA and 4-ABPA appeared to have agonist properties. 4. Phaclofen, 2-hydroxysaclofen, 3-APPA and 9G seemed to have little effect in this system at the doses tested. 5. Differences between in vivo and in vitro activity could be explained by differences in blood-brain barrier permeability, or possible differences in affinities for the sub-classes of GABAB receptors.
- Subjects :
- Animals
Baclofen analogs & derivatives
Baclofen antagonists & inhibitors
Baclofen pharmacology
Drug Interactions
Female
Ligands
Mice
Mice, Inbred BALB C
Muscle Relaxation drug effects
Organophosphorus Compounds pharmacology
beta-Alanine analogs & derivatives
beta-Alanine pharmacology
GABA Antagonists pharmacology
GABA-B Receptor Antagonists
Subjects
Details
- Language :
- English
- ISSN :
- 0306-3623
- Volume :
- 26
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- General pharmacology
- Publication Type :
- Academic Journal
- Accession number :
- 7590097
- Full Text :
- https://doi.org/10.1016/0306-3623(94)00175-m