Literature DB >> 2172872

Differential benzodiazepine pharmacology of mammalian recombinant GABAA receptors.

G von Blankenfeld1, S Ymer, D B Pritchett, H Sontheimer, M Ewert, P H Seeburg, H Kettenmann.   

Abstract

We compared gamma-aminobutyric acid (GABA)-activated currents and their modulation by benzodiazepines in cultured human cells transfected with complementary desoxyribonucleic acid (cDNA) encoding different GABAA receptor subunits. Flunitrazepam, a benzodiazepine agonist which potentiates GABA responses in both neurons and astrocytes was only effective in receptors containing the gamma 2 subunit (alpha 1 beta 1 gamma 2 and alpha 5 beta 1 gamma 2). The beta-carboline methyl-4-ethyl-6,7-dimethoxy-beta-carboline-3-carboxylate (DMCM) decreased GABA-activated currents in receptors composed of alpha 1 beta 1 gamma 1 and alpha 1 beta 1 gamma 2 subunits but increased GABA-activated currents in receptors containing the alpha 5 subunit (alpha 5 beta 1 gamma 1 and alpha 5 beta 1 gamma 2). These results strongly suggest that flunitrazepam and DMCM do not act on isosteric sites and that differences in the responsiveness of GABAA receptors to these compounds are based on different subunit compositions of GABAA receptors.

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Year:  1990        PMID： 2172872     DOI： 10.1016/0304-3940(90)90467-n

Source DB:  PubMed          Journal:  Neurosci Lett        ISSN： 0304-3940            Impact factor:   3.046


  9 in total

1.  Altered ratios of alternatively spliced long and short gamma2 subunit mRNAs of the gamma-amino butyrate type A receptor in prefrontal cortex of schizophrenics.

Authors:  M M Huntsman; B V Tran; S G Potkin; W E Bunney; E G Jones
Journal:  Proc Natl Acad Sci U S A       Date:  1998-12-08       Impact factor: 11.205

2.  GABA(A) receptors containing (alpha)5 subunits in the CA1 and CA3 hippocampal fields regulate ethanol-motivated behaviors: an extended ethanol reward circuitry.

Authors:  H L June; S C Harvey; K L Foster; P F McKay; R Cummings; M Garcia; D Mason; C Grey; S McCane; L S Williams; T B Johnson; X He; S Rock; J M Cook
Journal:  J Neurosci       Date:  2001-03-15       Impact factor: 6.167

Review 3.  Glutamate and GABA receptors in vertebrate glial cells.

Authors:  G von Blankenfeld; H Kettenmann
Journal:  Mol Neurobiol       Date:  1991       Impact factor: 5.590

Review 4.  A review of evidence for GABergic predominance/glutamatergic deficit as a common etiological factor in both schizophrenia and affective psychoses: more support for a continuum hypothesis of "functional" psychosis.

Authors:  R F Squires; E Saederup
Journal:  Neurochem Res       Date:  1991-10       Impact factor: 3.996

5.  Human neuronal gamma-aminobutyric acid(A) receptors: coordinated subunit mRNA expression and functional correlates in individual dentate granule cells.

Authors:  A R Brooks-Kayal; M D Shumate; H Jin; D D Lin; T Y Rikhter; K L Holloway; D A Coulter
Journal:  J Neurosci       Date:  1999-10-01       Impact factor: 6.167

6.  Clozapine's antipsychotic effects do not depend on blockade of 5-HT3 receptors.

Authors:  R F Squires; E Saederup
Journal:  Neurochem Res       Date:  1999-05       Impact factor: 3.996

7.  "Anxiolytic" and "anxiogenic" benzodiazepines and beta-carbolines: effects on aggressive and social behavior in rats and squirrel monkeys.

Authors:  E M Weerts; W Tornatzky; K A Miczek
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

Review 8.  The diversity of GABAA receptors. Pharmacological and electrophysiological properties of GABAA channel subtypes.

Authors:  W Hevers; H Lüddens
Journal:  Mol Neurobiol       Date:  1998-08       Impact factor: 5.590

9.  Direct modulation of GABAA receptor by intracellular ATP in dissociated nucleus tractus solitarii neurones of rat.

Authors:  T Shirasaki; K Aibara; N Akaike
Journal:  J Physiol       Date:  1992-04       Impact factor: 5.182
  9 in total

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