Literature DB >> 8931105

Gamma hydroxybutyrate is not a GABA agonist.

J J Feigenbaum1, S G Howard.   

Abstract

Gamma hydroxybutyrate (GHB) is primarily known and used as a relatively specific inhibitor of central DA release. However, it is also widely assumed to be an agonist or prodrug of gamma-aminobutyric acid (GABA) and its central activity has been attributed to an action exerted at GABA receptors. Nevertheless, there is compelling evidence that: (1) GHB formation may occur independently of GABA; (2) GHB is behaviorally, biochemically and physiologically distinct from GABA in many ways, and does not consistently effect GABAA or GABAB agonist induced responses; (3) GHB has little effect on either GABAA or GABAB receptors at less than millimolar concentrations. Consequently, GHB does not appear to be either a GABA prodrug or a GABA agonist. However, the GHB metabolite gamma butyrolactone (GBL) may possess some limited GABA agonist activity.

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Year:  1996        PMID: 8931105     DOI: 10.1016/0301-0082(96)00029-9

Source DB:  PubMed          Journal:  Prog Neurobiol        ISSN: 0301-0082            Impact factor:   11.685


  7 in total

1.  gamma-aminobutyric acid type B receptors are expressed and functional in mammalian cardiomyocytes.

Authors:  P Lorente; A Lacampagne; Y Pouzeratte; S Richards; B Malitschek; R Kuhn; B Bettler; G Vassort
Journal:  Proc Natl Acad Sci U S A       Date:  2000-07-18       Impact factor: 11.205

Review 2.  Neurosteroids, GABAA receptors, and ethanol dependence.

Authors:  Paolo Follesa; Francesca Biggio; Giuseppe Talani; Luca Murru; Mariangela Serra; Enrico Sanna; Giovanni Biggio
Journal:  Psychopharmacology (Berl)       Date:  2005-09-15       Impact factor: 4.530

3.  Changes in GABA(A) receptor gene expression associated with selective alterations in receptor function and pharmacology after ethanol withdrawal.

Authors:  Enrico Sanna; Maria Cristina Mostallino; Fabio Busonero; Giuseppe Talani; Stefania Tranquilli; Manuel Mameli; Saturnino Spiga; Paolo Follesa; Giovanni Biggio
Journal:  J Neurosci       Date:  2003-12-17       Impact factor: 6.167

4.  Effects of GABA agonists on body temperature regulation in GABA(B(1))-/- mice.

Authors:  Christophe Quéva; Marianne Bremner-Danielsen; Anders Edlund; A Jonas Ekstrand; Susanne Elg; Sven Erickson; Thore Johansson; Anders Lehmann; Jan P Mattsson
Journal:  Br J Pharmacol       Date:  2003-08-11       Impact factor: 8.739

Review 5.  Benefits and risks of pharmacotherapy for narcolepsy.

Authors:  Merrill M Mitler; Roza Hayduk
Journal:  Drug Saf       Date:  2002       Impact factor: 5.606

6.  Mild reduction in the activity of the alpha-ketoglutarate dehydrogenase complex elevates GABA shunt and glycolysis.

Authors:  Qingli Shi; Øystein Risa; Ursula Sonnewald; Gary E Gibson
Journal:  J Neurochem       Date:  2009-05       Impact factor: 5.372

Review 7.  GHB pharmacology and toxicology: acute intoxication, concentrations in blood and urine in forensic cases and treatment of the withdrawal syndrome.

Authors:  Francesco P Busardò; Alan W Jones
Journal:  Curr Neuropharmacol       Date:  2015-01       Impact factor: 7.363

  7 in total

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