The GABAB Receptor Profile of a Series of Phosphinic Acids: Agonist and Antagonist Activity in a Range of Peripheral Tissues

  • J. M. Hills
  • W. Howson


In the CNS, baclofen, a GABA analogue now known to interact with GABA receptors, was shown early on to have distinctly different effects from GABA (Fig. 1) [7]. These differences were highlighted by the work of Bowery and collegues, who showed that the baclofen induced repression of transmitter release from CNS tissue in vitro could not be blocked [11], and that a proportion of 3H-GABA binding to brain membranes was not displaced [18] by the GABA antagonist bicuculline. It was proposed that a second class of GABA receptors, selectively activated by baclofen and insensitive to antagonism by bicuculline, may exist in the mammalian brain. The classical GABA receptor became known as the GABAA receptor, whereas the new bicuculline insensitve receptor was termed the GABAB receptor.


GABAs Receptor GABAB Receptor Phosphonic Acid Phosphinic Acid GABAB Agonist 
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© Springer-Verlag Berlin Heidelberg 1992

Authors and Affiliations

  • J. M. Hills
  • W. Howson

There are no affiliations available

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