Abstract
NEUROTRANSMITTER receptors might be identified biochemically in binding studies with synaptic membrane preparations using labelled receptor agonists or antagonists as ligands1. In attempts to identify the GABA receptor 3H-GABA has been used as ligand. 3H-GABA, however, also binds to glial and neuronal GABA uptake sites and to enzymes metabolising GABA. Thus, Na+-dependent 3H-GABA-binding2,3, in contrast to Na+-independent 3H-GABA-binding is possibly not related to the GABA receptor4. In the present investigation the GABA antagonist 3H( + )bicuculline–methiodide (3H( + )BM) was used as ligand, which in contrast to bicuculline, is chemically sufficiently stable5. ( + )Bicuculline and its N-methyl-derivative antagonise reversibly and rather selectively the inhibitory synaptic action of GABA in the central nervous system (CNS) (refs 6, 7) without affecting the uptake or release of GABA or enzymes metabolising GABA (refs 8, 9). Thus 3H( + )BM might be more suitable for GABA receptor binding studies than GABA itself.
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References
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MÖHLER, H., OKADA, T. GABA receptor binding with 3H (+) bicuculline–methiodide in rat CNS. Nature 267, 65–67 (1977). https://doi.org/10.1038/267065a0
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DOI: https://doi.org/10.1038/267065a0
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