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https://www.readbyqxmd.com/read/29031482/toxicologic-transport-properties-of-ncs-382-a-%C3%AE-hydroxybutyrate-ghb-receptor-ligand-in-neuronal-and-epithelial-cells-therapeutic-implications-for-ssadh-deficiency-a-gaba-metabolic-disorder
#1
K R Vogel, G R Ainslie, A McConnell, J-B Roullet, K M Gibson
We report the in vitro assessment of pharmacotoxicity for the high-affinity GHB receptor ligand, NCS-382, using neuronal stem cells derived from mice with a targeted deletion of the aldehyde dehydrogenase 5a1 gene (succinic semialdehyde dehydrogenase(SSADH)-deficient mice). These animals represent a phenocopy of the human disorder of GABA metabolism, SSADH deficiency, that metabolically features accumulation of both GABA and the GABA-analog γ-hydroxybutyric acid in conjunction with a nonspecific neurological phenotype...
October 12, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/29028338/molecular-hybridization-of-potent-and-selective-%C3%AE-hydroxybutyric-acid-ghb-ligands-design-synthesis-binding-studies-and-molecular-modelling-of-novel-3-hydroxycyclopent-1-enecarboxylic-acid-hocpca-and-trans-%C3%AE-hydroxycrotonic-acid-t-hca-analogs
#2
Jacob Krall, Claus Hatt Jensen, Francesco Bavo, Christina Birkedal Falk-Petersen, Anne Stahr Haugaard, Stine Byskov Vogensen, Yongsong Tian, Mia Nittegaard-Nielsen, Sara Björk Sigurdardóttir, Jan Kehler, Kenneth Thermann Kongstad, David E Gloriam, Rasmus Prætorius Clausen, Kasper Harpsøe, Petrine Wellendorph, Bente Frølund
γ-hydroxybutyric acid (GHB) is a neuroactive substance with specific high-affinity binding sites. To facilitate target identification and ligand optimization, we herein report a comprehensive structure-affinity relationship study for novel ligands targeting these binding sites. A molecular hybridization strategy was used based on the conformationally restricted 3-hydroxycyclopent-1-enecarboxylic acid (HOCPCA) and the linear GHB analog, trans-4-hydroxycrotonic acid (T-HCA). In general, all structural modifications performed on HOCPCA led to reduced affinity...
October 13, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28938889/intoxication-with-ghb-gbl-characteristics-and-trends-from-ambulance-attended-overdoses
#3
Desiree Madah-Amiri, Lars Myrmel, Guttorm Brattebø
BACKGROUND: Overdoses from so-called "club drugs" (GHB/GBL) have become a more frequent cause of overdoses attended by ambulance services. Given its availability, affordability, and lack of awareness of risks, there is a common misconception among users that the drug is relatively safe. METHODS: This study reviewed ambulance records in Bergen, Norway between 2009 and 2015 for cases of acute poisonings, particularly from suspected GHB/GBL intoxication. RESULTS: In total, 1112 cases of GHB and GBL poisoning were identified...
September 22, 2017: Scandinavian Journal of Trauma, Resuscitation and Emergency Medicine
https://www.readbyqxmd.com/read/28869822/potential-of-ghb-phase-ii-metabolites-to-complement-current-approaches-in-ghb-post-administration-detection
#4
Thomas Piper, Lena-Maria Mehling, Annika Spottke, Anna Heidbreder, Peter Young, Burkhard Madea, Cornelius Hess, Wilhelm Schänzer, Mario Thevis
Recently, phase-II-metabolites of γ-hydroxybutyric acid (GHB), namely GHB-β-O-glucuronide and GHB-4-sulfate, were implemented in the scope of drug testing methods The clearance of GHB from the circulation is extremely fast due to its incorporation into the metabolic pathway of the citrate cycle. The elimination half-life of GHB from blood was reported to be dose dependent between 30 and 50min resulting in narrow detection windows of less than 12h after illicit administration or cases of drug facilitated sexual assault regardless of the biological matrix used...
October 2017: Forensic Science International
https://www.readbyqxmd.com/read/28844014/changes-in-smoking-status-among-a-longitudinal-cohort-of-gay-bisexual-and-other-men-who-have-sex-with-men-in-vancouver-canada
#5
Helia Shariati, Heather L Armstrong, Zishan Cui, Nathan J Lachowsky, Julia Zhu, Praney Anand, Eric A Roth, Robert S Hogg, Greg Oudman, Christina Tonella, David M Moore
BACKGROUND: Cigarette smoking is common among gay, bisexual, and other men who have sex with men (GBMSM) and most of the mortality gap between HIV-positive and HIV-negative individuals is attributable to smoking. METHODS: We recruited sexually active HIV-positive and HIV-negative GBMSM age ≥16 years using respondent-driven sampling. Study visits occurred every six months for up to four years and included a computer-assisted self-interview and clinical assessment...
August 16, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28830220/exploring-strategies-for-prep-adherence-and-dosing-preferences-in-the-context-of-sexualized-recreational-drug-use-among-msm-a-qualitative-study
#6
Elizabeth F Closson, Jennifer A Mitty, Jowanna Malone, Kenneth H Mayer, Matthew J Mimiaga
The use of recreational drugs while having sex is associated with increased HIV incidence among men who have sex with men (MSM). Taking a daily antiretroviral pill, or pre-exposure prophylaxis (PrEP) is a biomedical intervention to prevent HIV. However, the efficacy of PrEP is closely tied with high levels of adherence. While PrEP has the potential to reduce HIV acquisition, the use of recreational drugs may impede adherence. We explored perceptions of PrEP utilization and regimen preferences among 40 HIV-negative, MSM who reported concurrent recreational drug use and condomless anal sex with a man...
August 22, 2017: AIDS Care
https://www.readbyqxmd.com/read/28811136/determination-of-ghb-and-ghb-%C3%AE-o-glucuronide-in-hair-of-three-narcoleptic-patients-comparison-between-single-and-chronic-ghb-exposure
#7
Lena-Maria Mehling, Xin Wang, Sys-Stybe Johansen, Annika Spottke, Anna Heidbreder, Peter Young, Burkhard Madea, Cornelius Hess
Gamma-hydroxybutyric acid (GHB) can be used as a knock-out drug in drug facilitated crime (DFC). Due to its rapid metabolism and resulting narrow detection window, uncovering GHB use in DFC still constitutes a problem. In this experiment we determined the GHB and GHB-β-O-glucuronide (GHB-Gluc) concentrations in hair samples after single and chronic GHB exposures. Hair samples of three narcoleptic patients therapeutically taking sodium oxybate (GHB-sodium-salt) were collected. Patients 1 (P1) and 2 (P2) took the medication for nine and six years, respectively...
September 2017: Forensic Science International
https://www.readbyqxmd.com/read/28763296/hair-testing-of-ghb-an-everlasting-issue-in-forensic-toxicology
#8
REVIEW
Francesco Paolo Busardò, Simona Pichini, Simona Zaami, Roberta Pacifici, Pascal Kintz
BACKGROUND: In this paper, the authors present a critical review of different studies regarding hair testing of endogenous γ-hydroxybutyrate (GHB), concentrations in chronic users, and values measured after a single GHB exposure in drug facilitated sexual assault (DFSA) cases together with the role of a recently identified GHB metabolite, GHB-glucuronide. CONTENT: The following databases (up to March 2017) PubMed, Scopus and Web of Science were used, searching the following key words: γ-hydroxybutyrate, GHB, GHB glucuronide, hair...
August 1, 2017: Clinical Chemistry and Laboratory Medicine: CCLM
https://www.readbyqxmd.com/read/28745845/sedative-hypnotic-drug-withdrawal-syndrome-recognition-and-treatment-digest
#9
Cynthia Santos, Ruben E Olmedo, Jeremy Kim
Sedative-hypnotic drugs include gamma-Aminobutyric acid (GABA)ergic agents such as benzodiazepines, barbiturates, gamma-Hydroxybutyric acid [GHB], gamma-Butyrolactone [GBL], baclofen, and ethanol. Chronic use of these substances can cause tolerance, and abrupt cessation or a reduction in the quantity of the drug can precipitate a life-threatening withdrawal syndrome. Benzodiazepines, phenobarbital, propofol, and other GABA agonists or analogues can effectively control symptoms of withdrawal from GABAergic agents...
March 22, 2017: Emergency Medicine Practice
https://www.readbyqxmd.com/read/28714673/direct-monitoring-of-exogenous-%C3%AE-hydroxybutyric-acid-in-body-fluids-by-nmr-spectroscopy
#10
Martina Palomino-Schätzlein, Yaoyao Wang, Alan D Brailsford, Teodor Parella, David A Cowan, Cristina Legido-Quigley, Míriam Pérez-Trujillo
γ-Hydroxybutyric acid (GHB) is a popular drug increasingly associated with cases of drug-facilitated sexual assault (DFSA). Currently, expanding procedures of analysis and having forensic evidence of GHB intake in a long term are mandatory. Up to now, most studies have been performed using GC/MS and LC-MS as analytical platforms, which involve significant manipulation of the sample and, often, indirect measurements. In this work, procedures used in NMR-based metabolomics were applied to a GHB clinical trial on urine and serum...
August 3, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28683403/monastrol-a-3-4-dihydropyrimidin-2-1h-thione-as-structural-scaffold-for-the-development-of-modulators-for-ghb-high-affinity-binding-sites-and-%C3%AE-1%C3%AE-2%C3%AE-gabaa-receptors
#11
Maria Damgaard, Anas Al-Khawaja, Mia Nittegaard-Nielsen, Rebekka F Petersen, Petrine Wellendorph, Bente Frølund
The α4βδ subtype of the γ-aminobutyric acid (GABA) type A receptors (GABAARs) has been shown to be implicated in high-affinity binding of the neuromodulator γ-hydroxybutyric acid (GHB), but may not be the only GHB high-affinity binding sites. Monastrol has been identified as a modulator of GHB high-affinity binding and is furthermore reported as an allosteric modulator selective for the α1β2δ GABAARs. Therefore, structural determinants for selectivity at the two targets were investigated. 39 structural diverse monastrol analogues were synthesized by employing the Biginelli cyclocondensation and examined for modulation of GHB high-affinity binding using the GHB-specific ligand [(3)H]NCS-382 [(E,RS)-6,7,8,9-tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylidene)acetic acid] in rat brain homogenate...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28668666/ghb-levels-in-breast-milk-of-women-with-narcolepsy-with-cataplexy-treated-with-sodium-oxybate
#12
Emily C Barker, Michelle Puchowicz, John Letterio, Kristine Higgins, Katherine M Sharkey
OBJECTIVE: To determine GHB levels in breast milk of women taking sodium oxybate (Xyrem) for treatment of narcolepsy and cataplexy. METHODS: Two women with narcolepsy and cataplexy treated with sodium oxybate before pregnancy collected breast milk for analysis of GHB concentration after resuming sodium oxybate postpartum. One woman collected samples across two consecutive nights (doses: 3.0 gm and 4.5 gm twice per night) five months after delivering her first child; the other collected samples on three separate days (doses: 2...
June 1, 2017: Sleep Medicine
https://www.readbyqxmd.com/read/28664505/ssadh-deficiency-in-an-italian-family-a-novel-aldh5a1-gene-mutation-affecting-the-succinic-semialdehyde-substrate-binding-site
#13
Sara Leo, Concetta Capo, Bianca Maria Ciminelli, Federico Iacovelli, Giovanna Menduti, Silvia Funghini, Maria Alice Donati, Mattia Falconi, Luisa Rossi, Patrizia Malaspina
SSADH deficiency (SSADHD) is a rare autosomal recessively inherited metabolic disorder. It is associated with mutations of ALDH5A1 gene, coding for the homotetrameric enzyme SSADH. This enzyme is involved in γ-aminobutyric acid (GABA) catabolism, since it oxidizes succinic semialdehyde (SSA) to succinate. Mutations in ALDH5A1 gene result in the abnormal accumulation of γ-hydroxybutyrate (GHB), which is pathognomonic of SSADHD. In the present report, diagnosis of SSADHD in a three-month-old female was achieved by detection of high levels of GHB in urine...
June 29, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28662343/effect-of-chronic-%C3%AE-hydroxybutyrate-ghb-administration-on-ghb-toxicokinetics-and-ghb-induced-respiratory-depression
#14
Bridget L Morse, Gurkishan S Chadha, Melanie A Felmlee, Kristin E Follman, Marilyn E Morris
BACKGROUND: γ-hydroxybutyrate (GHB) has a high potential for illicit use; overdose of this compound results in sedation, respiratory depression and death. Tolerance to the hypnotic/sedative and electroencephalogram effects of GHB occurs with chronic GHB administration; however, tolerance to respiratory depression has not been evaluated. GHB toxicodynamic effects are mediated predominantly by GABAB receptors. Chronic treatment may affect monocarboxylate transporters (MCTs) and alter the absorption, renal clearance and brain uptake of GHB...
June 29, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28653244/%C3%AE-hydroxybutyric-acid-ghb-pharmacokinetics-and-pharmacodynamics-semi-mechanistic-and-physiologically-relevant-pk-pd-model
#15
Rutwij A Dave, Kristin E Follman, Marilyn E Morris
An overdose of γ-hydroxybutyric acid (GHB), a drug of abuse, results in fatality caused by severe respiratory depression. In this study, a semi-mechanistic pharmacokinetic/pharmacodynamic (PK/PD) model was developed to characterize monocarboxylate transporter 1 (MCT1)-mediated transport of GHB, as well as effects of GHB on respiration frequency, for IV doses of 200, 600, and 1500 mg/kg in rats. The proposed PK/PD model for GHB consists of nonlinear metabolism of GHB in the liver, MCT1-mediated renal reabsorption with physiologically relevant concurrent fluid reabsorption, MCT1-mediated uptake into the brain, and direct effects of binding of GHB to GABAB receptors on the PD parameter, respiration frequency...
June 26, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28649510/targeted-screening-of-succinic-semialdehyde-dehydrogenase-deficiency-ssadhd-employing-an-enzymatic-assay-for-%C3%AE-hydroxybutyric-acid-ghb-in-biofluids
#16
C Wernli, S Finochiaro, C Volken, H Andresen-Streichert, A Buettler, D Gygax, G S Salomons, E E Jansen, G R Ainslie, K R Vogel, K M Gibson
HYPOTHESIS: An enzymatic assay for quantification of γ-hydroxybutyric acid (GHB) in biofluids can be employed for targeted screening of succinic semialdehyde dehydrogenase deficiency (SSADHD) in selected populations. RATIONALE: We used a two-tiered study approach, in which the first study (proof of concept) examined 7 urine samples derived from patients with SSADHD and 5 controls, and the second study (feasibility study) examined a broader sample population of patients and controls, including plasma...
June 2017: Molecular Genetics and Metabolism Reports
https://www.readbyqxmd.com/read/28627831/whole-blood-thiopurine-s-methyltransferase-genotype-and-phenotype-concordance-in-iranian-kurdish-ulcerative-colitis-uc-patients
#17
Fariborz Bahrehmand, Asad Vaisi-Raygani, Amir Kiani, Homayoun Bashiri, Mahdi Zobeiri, Maryam Tanhapour, Tayebeh Pourmotabbed
BACKGROUND: Thiopurine methyl transferase (TPMT), a drug-metabolizing enzyme, catalyzes methylation and consequently, the metabolism of thiopurine compounds used for treatment of inflammatory bowel disease (IBD). Individuals who are homozygous recessive or have extremely low TPMT activity need to avoid thiopurines because of concern for significant leukopenia. The aim of this research was to determine TPMT phenotypes and genotypes in IBD patients to predict the risk of thiopurine toxicity before treatment...
May 1, 2017: Clinical Laboratory
https://www.readbyqxmd.com/read/28602470/further-evidence-for-ghb-naturally-occurring-in-common-non-alcoholic-beverages
#18
Simon P Elliott, Paolo Fais
GHB has been implicated in many cases of suspected surreptitious administration with the purpose of increasing victim vulnerability to sexual assault. Low amounts of endogenous (or naturally occurring) GHB, which do not reach pharmacologically active levels, have been detected in alcoholic and non-alcoholic beverages. Due to the continued requirement to obtain data on the presence of endogenous GHB in various beverage types, GHB concentrations were measured in a series of non-alcoholic beverages. Tonic water and lemon flavoured tonic water beverages were analysed at 0, 24 and 96h after the bottle opening using gas chromatography coupled to tandem mass spectrometry (GC-MS/MS) on an Agilent 6890/7000C Triple Quadrupole...
May 20, 2017: Forensic Science International
https://www.readbyqxmd.com/read/28579487/intoxication-by-gamma-hydroxybutyrate-and-related-analogues-clinical-characteristics-and-comparison-between-pure-intoxication-and-that-combined-with-other-substances-of-abuse
#19
MULTICENTER STUDY
Òscar Miró, Miguel Galicia, Paul Dargan, Alison M Dines, Isabelle Giraudon, Fridtjof Heyerdahl, Knut E Hovda, Christopher Yates, David M Wood
OBJECTIVE: To study the profile of European gamma-hydroxybutyrate (GHB) and gammabutyrolactone (GBL) intoxication and analyse the differences in the clinical manifestations produced by intoxication by GHB/GBL alone and in combination with other substances of abuse. METHOD: We prospectively collected data on all the patients attended in the Emergency Departments (ED) of the centres participating in the Euro-DEN network over 12 months (October 2013 to September 2014) with a primary presenting complaint of drug intoxication (excluding ethanol alone) and registered the epidemiological and clinical data and outcomes...
August 5, 2017: Toxicology Letters
https://www.readbyqxmd.com/read/28561068/gamma-hydroxybutyrate-increases-resting-state-limbic-perfusion-and-body-and-emotion-awareness-in-humans
#20
Oliver G Bosch, Fabrizio Esposito, Michael M Havranek, Dario Dornbierer, Robin von Rotz, Philipp Staempfli, Boris B Quednow, Erich Seifritz
Gamma-hydroxybutyrate (GHB) is a GHB-/GABA-B receptor agonist inducing a broad spectrum of subjective effects including euphoria, disinhibition, and enhanced vitality. It is used as treatment for neuropsychiatric disorders including narcolepsy and alcohol withdrawal, but is also a drug of abuse. Non-medical users report enhancement of body and emotion awareness during intoxication. However, the neuronal underpinnings of such awareness alterations under GHB are unknown so far. The assessment of regional cerebral blood flow (rCBF) by pharmacological magnetic resonance imaging (phMRI) enables the elucidation of drug-induced functional brain alterations...
October 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
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