Bicuculline-insensitive GABA receptors: studies on the binding of (-)-baclofen to rat cerebellar membranes

The binding of [3H](-)-baclofen to synaptic membranes prepared from rat cerebellum was studied. Consistent with pharmacological data that (-)-baclofen is the more active stereoisomer, studies on the binding of [3H](-)-baclofen showed increased specific binding, a higher affinity Kd and a lower Bmax...

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Bibliographic Details
Published inNeuroscience letters Vol. 52; no. 3; p. 317
Main Authors Drew, C A, Johnston, G A, Weatherby, R P
Format Journal Article
LanguageEnglish
Published Ireland 21.12.1984
Subjects
Animals
Baclofen - metabolism
Bicuculline - pharmacology
Cations, Divalent - pharmacology
Cerebellum - metabolism
gamma-Aminobutyric Acid - analogs & derivatives
gamma-Aminobutyric Acid - pharmacology
Kinetics
Rats
Receptors, GABA-A - drug effects
Receptors, GABA-A - metabolism
Synaptic Membranes - metabolism
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Summary:The binding of [3H](-)-baclofen to synaptic membranes prepared from rat cerebellum was studied. Consistent with pharmacological data that (-)-baclofen is the more active stereoisomer, studies on the binding of [3H](-)-baclofen showed increased specific binding, a higher affinity Kd and a lower Bmax than equivalent studies using [3H](+/-)-baclofen. Divalent metal ions (mercury, lead, calcium and zinc) inhibited the binding of [3H](-)-baclofen. The effects of some conformationally restricted analogues of gamma-aminobutyric acid (GABA) on [3H](-)-baclofen binding indicated that GABA interacts with (-)-baclofen-sensitive binding sites (GABAB) in extended rather than folded conformations, and that folded analogues of GABA may interact with a class of binding site (GABAc?) insensitive to (-)-baclofen and bicuculline.
ISSN:0304-3940
DOI:10.1016/0304-3940(84)90181-2