Hydroxybutyrates

Publication Title: 
Psychoneuroendocrinology

Gamma-hydroxybutyrate (GHB) is a GHB-/GABAB-receptor agonist. Reports from GHB abusers indicate euphoric, prosocial, and empathogenic effects of the drug. We measured the effects of GHB on mood, prosocial behavior, social and non-social cognition and assessed potential underlying neuroendocrine mechanisms. GHB (20mg/kg) was tested in 16 healthy males, using a randomized, placebo-controlled, cross-over design. Subjective effects on mood were assessed by visual-analogue-scales and the GHB-Specific-Questionnaire.

Author(s): 
Bosch, Oliver G.
Eisenegger, Christoph
Gertsch, J¸rg
von Rotz, Robin
Dornbierer, Dario
Gachet, M. SalomÈ
Heinrichs, Markus
Wetter, Thomas C.
Seifritz, Erich
Quednow, Boris B.
Publication Title: 
The Journal of Pharmacology and Experimental Therapeutics

The pharmacokinetics of sodium-gamma-hydroxybutyrate (NaGHB) have been examined as functions of dose and route of administration. The elimination of NaGHB appeared to be controlled by a capacity-limited process which can be described by Michaelis-Menten kinetics.

Author(s): 
Lettieri, J. T.
Fung, H. L.
Publication Title: 
Neuropharmacology
Author(s): 
Winters, W. D.
Kott, K. S.
Publication Title: 
Psychopharmacology

RATIONALE: A recent in-vitro study demonstrated that the potent disulfide reducing agent, DL-dithiothreitol (DTT), may alter the structural stability of the GABA(B) receptor, probably inactivating the disulfide bonds between four cysteine residues located in the GABA(B1(a)) receptor structure. OBJECTIVES: The present study was designed to evaluate whether DTT treatment was capable of antagonizing some behavioral effects of pharmacological stimulation of the GABA(B) receptor.

Author(s): 
Carai, Mauro A. M.
Vacca, Giovanni
Serra, Salvatore
Colombo, Giancarlo
Froestl, Wolfgang
Gessa, Gian Luigi
Publication Title: 
Brain Research

The present study investigated whether the differential sensitivity of selectively bred gamma-hydroxybutyric acid (GHB)-sensitive (GHB-S) and GHB-resistant (GHB-R) rats to GHB- and baclofen-induced sedation/hypnosis generalized to the motor incoordinating effect of the two drugs. To this aim, GHB-S and GHB-R rats were tested on a Rota-Rod after the acute administration of GHB (100-500 mg/kg, i.p.) and baclofen (1.25-5 mg/kg, i.p.).

Author(s): 
Lobina, Carla
Colombo, Giancarlo
Gessa, Gian Luigi
Carai, Mauro A. M.
Publication Title: 
Drug and Alcohol Dependence

Gamma-hydroxybutyrate (GHB), a metabolite of GABA, is a drug of abuse and a therapeutic. The illicit use of GHB precursors and analogs reportedly has increased worldwide. Gamma-hydroxyvaleric (GHV) is a 4-methyl-substituted analog of GHB that reportedly is abused and is marketed as a dietary supplement and replacement for GHB. The purpose of these studies was to compare the pharmacological and behavioral profiles of GHV and GHB.

Author(s): 
Carter, Lawrence P.
Chen, Weibin
Wu, Huifang
Mehta, Ashok K.
Hernandez, R. Jason
Ticku, Maharaj K.
Coop, Andrew
Koek, Wouter
France, Charles P.
Publication Title: 
Neuropharmacology

In the rat brain, gamma-hydroxybutyric-acid (GHB) increases the concentrations of 3alpha-hydroxy,5alpha-pregnan-20-one (allopregnanolone, 3alpha,5alpha-THP) and 3alpha,21-dihydroxy,5alpha-pregnan-20-one (allotetrahydrodeoxycorticosterone/3alpha,5alphaTHDOC), two neurosteroids acting as positive allosteric modulators of gamma-aminobutyric acid (GABA)(A) receptors. This study was aimed at assessing whether neurosteroids play a role in GHB-induced loss of righting reflex (LORR).

Author(s): 
Barbaccia, Maria Luisa
Carai, Mauro A. M.
Colombo, Giancarlo
Lobina, Carla
Purdy, Robert H.
Gessa, Gian Luigi
Publication Title: 
Mini Reviews in Medicinal Chemistry

Gamma hydroxybutyric acid (GHB), an endogenous constituent of the mammalian brain, acts as i) a neurotransmitter or neuromodulator, ii) a medicine used for the treatment of narcolepsy and alcoholism, and iii) a drug illicitly used for its psychotropic effects. GHB is thought to act as a specific GHB receptor agonist as well as a weak gamma-aminobutyric acid type B (GABA(B)) receptor agonist. Here, I review the in vivo and in vitro pharmacological properties of GHB and its interaction with GHB and GABA(B) receptors.

Author(s): 
Castelli, M. Paola
Publication Title: 
Journal of Chromatography. A

Gamma-hydroxybutyric acid is an emerging drug of abuse. Beside relaxation and euphoria it causes hypnosis and unconsciousness. Therefore the substance is misused as recreational drug and at drug-facilitated sexual assaults. An automated and effortless method for quantitation of gamma-hydroxybutyric acid in serum and urine was optimized and validated. Five hundred microliters sample volume are used for both matrices. The acid catalyzed conversion of gamma-hydroxybutyric acid to the corresponding gamma-butyrolactone is applied.

Author(s): 
Lenz, Daniel
Kröner, Lars
Rothschild, Markus A.
Publication Title: 
The Journal of Clinical Investigation

To assess the effect of each dietary caloric source on the catabolism of branched-chain amino acids, we investigated the rate of leucine oxidation before and after obese volunteers consumed one of the following diets for one week: (a) starvation, (b) 300 or 500 cal of fat/d, (c) 300 or 500 cal of carbohydrate/d, (d) 300 or 500 cal of protein/d, (e) a mixture of carbohydrate (300 cal/d) and fat (200 cal/d), or (f) a mixture of carbohydrate (300 cal/d) and protein (200 cal/d). Starvation significantly increased the rate of leucine oxidation (1.4 +/- 0.11 vs.

Author(s): 
Vazquez, J. A.
Morse, E. L.
Adibi, S. A.
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