Part of the pharmacological actions of&lt;/strong&gt; γ&lt;strong&gt;-hydroxybutyrate are mediated by GABA&lt;/strong&gt;&lt;sub&gt;&lt;strong&gt;B&lt;/strong&gt;&lt;/sub&gt; &lt;strong&gt;receptors

Bernasconi, R.; Mathivet, Pascal; Otten, U.; Settler, B; Bischoff, Stephan C.; Marescaux, Christian

doi:10.4324/9780203300992_chapter_3

Cited by 15 publications

(17 citation statements)

References 1 publication

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“…The present findings also strengthen the hypothesis that the pharmacologic effects produced by high doses of GHB are mediated by activation of the GABA B receptor. 22 The results of this study are in agreement with those recently reported by Gupta et al, 18 who found that the survival rate of SSADH-deficient mice was significantly increased by continuous exposure to the GABA B receptor antagonist CGP 35348.…”

Section: Discussionsupporting

confidence: 94%

Resuscitative Effect of a γ-Aminobutyric Acid B Receptor Antagonist on γ-Hydroxybutyric Acid Mortality in Mice

Carai

Colombo

Gessa

2005

Annals of Emergency Medicine

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Section: Discussionsupporting

confidence: 94%

Resuscitative Effect of a γ-Aminobutyric Acid B Receptor Antagonist on γ-Hydroxybutyric Acid Mortality in Mice

Carai

Colombo

Gessa

2005

Annals of Emergency Medicine

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“…The best-characterized GHBR ligand is NCS-382 which, as well as displacing GHB in binding studies, was shown to antagonize GABA B -independent GHB effects at least in a limited number of studies (described in the following sections). Several GHB analogs have also been produced (reviewed in 99,100), but there is very little evidence, in vivo or in vitro, that these compounds activate the putative GHBR (i.e., that they mimick GABA B -independent effects of GHB).…”

Section: Brain Targets Of Ghb: Molecular Biochemical and Pharmacolomentioning

confidence: 99%

A Critical Evaluation of the Gamma‐Hydroxybutyrate (GHB) Model of Absence Seizures

2014

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Typical absence seizures (ASs) are nonconvulsive epileptic events which are commonly observed in pediatric and juvenile epilepsies and may be present in adults suffering from other idiopathic generalized epilepsies. Our understanding of the pathophysiological mechanisms of ASs has been greatly advanced by the availability of genetic and pharmacological models, in particular the γ-hydroxybutyrate (GHB) model which, in recent years, has been extensively used in studies in transgenic mice. GHB is an endogenous brain molecule that upon administration to various species, including humans, induces not only ASs but also a state of sedation/hypnosis. Analysis of the available data clearly indicates that only in the rat does there exist a set of GHB-elicited behavioral and EEG events that can be confidently classified as ASs. Other GHB activities, particularly in mice, appear to be mostly of a sedative/hypnotic nature: thus, their relevance to ASs requires further investigation. At the molecular level, GHB acts as a weak GABA-B agonist, while the existence of a GHB receptor remains elusive. The pre- and postsynaptic actions underlying GHB-elicited ASs have been thoroughly elucidated in thalamus, but little is known about the cellular/network effects of GHB in neocortex, the other brain region involved in the generation of ASs.

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“…The endogenous brain levels of GHB (2-5 nmol/g) are believed to be too low to stimulate GABA B receptors (K i between 80 and 120 µM), although the synaptic cleft concentration is not known (42). Cortical GHB concentrations approaching 250 nmol/g, which are sufficient to stimulate GABA B receptors have been obtained by administration of 100-400 mg/kg of exogenous GHB (43).…”

Section: Table 4 Composition Of Molecular Species Of Dnph-derivatizedmentioning

confidence: 99%

1‐O‐alkyl‐2‐(ω‐oxo)acyl‐sn‐glycerols from shark oil and human milk fat are potential precursors of PAF mimics and GHB

Hartvigsen

Ravandi

Harkewicz

et al. 2006

Lipids

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This study examines the feasibility that peroxidation and lipolysis of 1-O-alkyl-2,3-diacyl-sn-glycerols (DAGE) found in shark liver oil and human milk fat constitutes a potential source of dietary precursors of platelet activating factor (PAF) mimics and of gamma-hydroxybutyrate (GHB). Purified DAGE were converted into 1-O-alkyl-2-acyl-sn-glycerols by pancreatic lipase, without isomerization, and transformed into 1-O-alkyl-2-oxoacyl-sn-glycerols by mild autooxidation. The various core aldehydes without derivatization, as well as the corresponding dinitrophenylhydrazones, were characterized by chromatographic retention time and diagnostic ions by online electrospray mass spectrometry. Core aldehydes of oxidized shark liver oil yielded 23 molecular species of 1-O-alkyl-sn-glycerols with short-chain sn-2 oxoacyl groups, ranging from 4 to 13 carbons, some unsaturated. Autooxidation of human milk fat yielded 1-O-octadecyl-2-(9-oxo)nonanoyl-sn-glycerol, as the major core aldehyde. Because diradylglycerols with short fatty chains are absorbed in the intestine and react with cytidine diphosphate-choline in the enterocytes, it is concluded that formation of such PAF mimics as 1-O-alkyl-2-(omega-oxo)acyl-sn-glycerophosphocholine from unsaturated dietary DAGE is a realistic possibility. Likewise, a C4 core alcohol produced by aldol-keto reduction of a C4 core aldehyde constitutes a dietary precursor of the neuromodulator and recreational drug GHB, which has not been previously pointed out.

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Part of the pharmacological actions of</strong> γ<strong>-hydroxybutyrate are mediated by GABA</strong><sub><strong>B</strong></sub> <strong>receptors

Cited by 15 publications

References 1 publication

Resuscitative Effect of a γ-Aminobutyric Acid B Receptor Antagonist on γ-Hydroxybutyric Acid Mortality in Mice

Resuscitative Effect of a γ-Aminobutyric Acid B Receptor Antagonist on γ-Hydroxybutyric Acid Mortality in Mice

A Critical Evaluation of the Gamma‐Hydroxybutyrate (GHB) Model of Absence Seizures

1‐O‐alkyl‐2‐(ω‐oxo)acyl‐sn‐glycerols from shark oil and human milk fat are potential precursors of PAF mimics and GHB

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