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

@article{Drew1984BicucullineinsensitiveGR,
  title={Bicuculline-insensitive GABA receptors: Studies on the binding of (−)-baclofen to rat cerebellar membranes},
  author={Colleen A. Drew and Graham A. R. Johnston and Robert P. Weatherby},
  journal={Neuroscience Letters},
  year={1984},
  volume={52},
  pages={317-321}
}

Bicuculline‐ and Baclofen‐Insensitive γ‐Aminobutyric Acid Binding to Rat Cerebellar Membranes

Abstract: Up to 60% of γ‐[3H]aminobutyric acid ([3H]GABA) bound specifically to rat cerebellar membranes in the absence of Ca2+ was insensitive to the GABAA antagonist bicuculline and to the GABAB

Molecular Biology, Pharmacology, and Physiology of GABAC Receptors

The first edition of The GABA Receptors (Enna, 1983) made no reference to the subtype of GABA receptors now known as GABAC receptors, i.e., receptors for the inhibitory neurotransmitter GABA that are

Changes in extracellular K+ evoked by GABA, THIP and baclofen in the guinea-pig hippocampal slice

TLDR
The K+ changes evoked by GABA appear to be mediated by the activation of GABAA receptors with low affinity and to be related to their depolarizing action, which suggests an outward counter/co-transport of K+ with Cl/HCO3 anion shifts and/or activation of a voltage-dependent K+ conductance.

Pharmacology of GABA pl and GABA a/fB receptors expressed in Xenopus oocytes and COS cells

TLDR
The findings suggest that the pl receptor recognizes agonists in the extended conformation, in contrast to GABAA receptors, which are believed to recognize agonist in the partially folded conformation.
...

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It is reported that high-affinity saturable binding of 3H-baclof en and3H-G AB A to the GABAB site can be detected in fragments of crude synaptic membranes prepared from rat brain and that GABA and baclofen can compete for the same recognition site.

(–)Baclofen decreases neurotransmitter release in the mammalian CNS by an action at a novel GABA receptor

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GABA clearly decreased the evoked release of accumulated 3H-noradrenaline from rat atria in vitro and3H-acetylcholine from preganglionic terminals in the rat superior cervical ganglion in vitro without affecting the basal release of tritium.

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Experimental findings are in very good agreement with Monte Carlo simulations and may help to explain the discrepancies in dissociation constants of high-affinity racemic radioligands reported in the literature.

The Synthesis and Activity of cis‐and trans‐2‐(Aminomethyl) cyclopropanecarboxylic Acid as Conformationally Restricted Analogues of GABA

TLDR
Both cyclopropane isomers inhibited the sodium‐independent binding of GABA to synaptic membranes from rat brain and their relative potencies were broadly consistent with the activity observed for these compounds in vivo on cat spinal neurons, reinforcing the evidence that extended rather than folded conformations of GABA are active at most GABA recognition sites within the mammalian central nervous system.

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TLDR
Trans‐4‐aminocrotonic acid, an analogue of GABA in an extended conformation, acts as efficiently as GABA with respect to each of the above systems, indicating that extended rather than folded conformations of GABA are likely to be important in the interaction of GABA with the specific macromolecules concerned.