*  Mutational analysis of molecular requirements for the actions of general anaesthetics at the γ-aminobutyric acidA receptor...
BACKGROUND: Amino acids in the beta subunit contribute to the action of general anaesthetics on GABA(A) receptors. We have now characterized the phenotypic effect of two beta subunit mutations in the most abundant GABA(A) receptor subtype, alpha1beta2gamma2. RESULTS: The beta2(N265M) mutation in M2 decreased the modulatory actions of propofol, etomidate and enflurane, but not of alphaxalone, while the direct actions of propofol, etomidate and alphaxalone were impaired. The beta2(M286W) mutation in M3 decreased the modulatory actions of propofol, etomidate and enflurane, but not of alphaxalone, whereas the direct action of propofol and etomidate, but not of alphaxalone, was impaired. CONCLUSIONS: We found that the actions of general anaesthetics at alpha1beta2(N265M)gamma2 and alpha1beta2(M286W)gamma2 GABA(A) receptors are similar to those previously observed at alpha2beta3(N265M)gamma2 and alpha2beta3(M286W)gamma2 ...
  http://www.zora.uzh.ch/id/eprint/875/
*  Effectiveness of GABA Agonists in Reducing the Reinforcing Effects of Cocaine - Full Text View - ClinicalTrials.gov
Cocaine likely creates its reinforcing and addictive effects by increasing levels of dopamine, a brain neurotransmitter. GABA agonists are chemicals that have the opposite effect by inhibiting the release of dopamine. Increasing GABA activity may result in greater inhibition of dopamine systems, which may lead to new treatments for cocaine abuse. The purpose of this study is to determine whether pretreatment with GABA agonists reduces the psychological and physiological reinforcing effects of cocaine. Specifically, the study will look at three different GABA agonists: tiagabine, baclofen, and trazolam.. This double-blind, placebo-controlled study will involve three separate experimental phases; each phase will last 4 weeks and will test one of three GABA agonists (tiagabine, baclofen, or trazolam). Daily testing sessions will last approximately 6 hours. One of four GABA agonist dose treatments will be ...
  https://clinicaltrials.gov/ct2/show/NCT00218166
*  Flavones and phenylpropanoids from a sedative extract of Lantana trifolia L. | Archivio della ricerca dell'Università degli...
The flavone glycosides, named scutellarein-7-O-β-d-apiofuranoside and apigenin-7-O-β-d-apiofuranosyl-(1 → 2)-β-d-apiofuranoside, and the flavone celtidifoline (5,6,4′,5′-tetrahydroxy-7,3′-dimethoxyflavone), along with other 11 known compounds, were isolated from leaves of the ethyl acetate extract of Lantana trifolia L. using step gradient High Speed Countercurrent Chromatography (HSCCC) and High Performance Liquid Chromatography (HPLC), respectively. Their structures were elucidated by spectroscopic methods, including 2D NMR and mass spectrometry (ESI-MS) techniques. The ethanolic and ethyl acetate extracts produced an intense sedative effect in mice, one hour after oral administration of 1 mg/kg. This effect was neither due to a benzodiazepine-like effect of the three flavone derivatives neither of the phenylpropanoids, betonyoside F and verbascoside, that were tested for their affinity for the [3H] flunitrazepam binding sites.. ...
  https://www.iris.unisa.it/handle/11386/3035836
*  Differential Effects of Neuroactive Steroids on Somatostatin and Dopamine Secretion from Primary Hypothalamic Cell Cultures -...
This study investigated the effects of neuroactive steroids, which have been reported to modulate GABA-ergic transmission, on the secretion of somatostatin (SRIH) and also dopamine (DA) from primary rat hypothalamic cell cultures, where the release of both substances is regulated by a GABAA receptor-mediated inhibitory tone. Pregnenolone sulphate (PS), a negative allosteric modulator at the GABAA receptor, enhanced SRIH secretion in a time and dose-dependent manner (10−12-10−8 M). This effect was reversed by muscimol (10−8 M) and enhanced by bicuculline (10−6 M), thus supporting an action of PS at the GABAA receptor. The release of endogenously synthesized dopamine (DA) was, however, unaffected by PS. A number of other steroids were also tested for their potential actions on SRIH and DA secretion. Allopregnanolone had slight but significant stimulatory actions on SRIH secretion, whereas tetrahydro-deoxycorticosterone (TH-DOC) markedly ...
  http://onlinelibrary.wiley.com/doi/10.1046/j.1365-2826.1997.00582.x/abstract?globalMessage=0
*  M&M Fitness Discount Supplements Australia - Other Amino Acid Supplements Australia | M&M Fitness
Buy the best amino supplements from M&M Fitness Australia supplement warehouse Brisbane. Buy amino acids such as phenibut (phenyl gamma aminobutyric acid), gaba (gamma aminobutyric acid), acetyl l-carnitine, agmatine, glycine, beta alanine and more! Order online or shop at our Brisbane supplement store with our huge range of discount supplements in Loganholme.
  https://www.mmfitness.com.au/australia/c77-Other-Amino-Acids/
*  UMR UNIS 1072 El far Debanne Goaillard Seagar Inserm neurobiologie hom ostasie excitabilit neuronale
Synaptic plasticity at excitatory glutamatergic synapses is believed to be instrumental in the maturation of neuronal networks. Using whole-cell patch-clamp recordings, we have studied the mechanisms of induction and expression of long-term depression at excitatory GABAergic synapses in the neonatal rat hippocampus (LTD(GABA-A)). We report that the induction of LTD(GABA-A) requires a GABA(A) receptor-mediated membrane depolarization, which is necessary to remove the Mg(2+) block from postsynaptic NMDA receptors. LTD(GABA-A) is associated with an increase in the coefficient of variation of evoked GABA(A) receptor-mediated synaptic currents and a decrease in the frequency, but not amplitude, of Sr(2+)-induced asynchronous GABA(A) quantal events. We conclude that LTD(GABA-A) induction requires the activation of both GABA(A) and NMDA ...
  http://unis-neuro.com/publications.php?id=229
*  AID 622165 - Positive allosteric modulation of AMPA receptor in Sprague-Dawley rat hippocampal neuron assessed as glutamate...
BioAssay record AID 622165 submitted by ChEMBL: Positive allosteric modulation of AMPA receptor in Sprague-Dawley rat hippocampal neuron assessed as glutamate-induced response pre-treated for 20 secs by patch-clamp electrophysiology.
  https://pubchem.ncbi.nlm.nih.gov/bioassay/622165
*  GABA and GABAAreceptor expression on immune cells in psoriasis: a pathophysiological role | SpringerLink
Psoriasis is a chronic inflammatory disease in which pruritus is a common symptom. Pruritus may be associated with the gamma-aminobutyric acid (GABA) system. The distribution of GABA and its GABAA receptor (R) was studied in involved and non-involved psoriatic skin, as well as normal healthy control skin, using an immunohistochemistry technique. Pruritus was determined using a visual analog scale. Inflammatory cells immunoreactive for the GABA ligand and the GABAA R were increased (P , 0.01, respectively) in the involved skin. Cells stained for GABA ligand were mostly macrophages with some lymphocytes, while cells stained for GABAA R were macrophages, neutrophils or lymphocytes. There was a positive correlation when comparing GABA ligand (P = 0.05) and GABAA R (P , 0.05) expressing inflammatory cells, with pruritus. The GABA ligand and its ...
  https://link.springer.com/article/10.1007/s00403-010-1052-5
*  Plus it
The role of GABAergic systems, specifically GABAA and GABAB receptors, in mediating the stimulant actions of EtOH were investigated in FAST and SLOW selected mouse lines, and subsequently in B6 and D2 inbred strains (GABAB studies only). Consistent with work in earlier generations of these mice (Phillips et al., 1992), differential sensitivities between FAST and SLOW mice were observed in response to some GABAA ligands tested. However, the GABAA receptor antagonists, bicuculline and picrotoxin, did not selectively reduce the EtOH stimulant response. On the other hand, FAST and SLOW mice differed in locomotor responses to baclofen, and EtOH's stimulant effects in FAST mice were blocked by administration of this GABABagonist. These GABAB effects were replicated in D2 inbred mice that display high sensitivity to the stimulant actions of EtOH. Taken together, ...
  http://jpet.aspetjournals.org/content/287/2/606
*  5 Easy Facts About diabetic neuropathy in feet Described
When nerves become ill that raising a chemical understood as GABA may relax down swollen and irritable nerves and provide relief for individuals having a hard time with the symptoms of neuropathy, it appears. You can think of GABA as a brake pedal that decreases the signs of neuropathy. There is research that recommend the herbs valerian root and lemon balm may increase GABA hence applying the body's brake on escaped nerve discomfort. Valerian root may obstruct an enzyme understood as GABA-T that breaks down and reduces the effects of GABA in the nervous system. By obstructing the breakdown of GABA, valerian root may lengthen the braking result of GABA on the nerve and decrease neuropathy signs. Lemon Balm appears to increase the effect of GABA in a somewhat different way. Rather than obstructing the breakdown of GABA, Lemon Balm may stimulate an enzyme ...
  http://deancpal791468.mybjjblog.com/5-easy-facts-about-diabetic-neuropathy-in-feet-described-2170205
*  Plus it
This study describes for the first time the identification of low-molecular-weight organic compounds that act as positive allosteric modulators at GABAB receptors in a native environment (rat brain membranes, neuronal cultures) or in recombinant expression systems (stably or transiently transfected mammalian cell lines, X. laevis oocytes).. The compound CGP7930, structurally close to the general anesthetic propofol, and its aldehyde analog CGP13501 potentiated GABA-induced signals in a functional receptor test (GTPγ[35S] binding), using membranes from CHO cells stably expressing the GABAB receptor (Fig.2). The findings that these signals exceeded the response elicited by a maximally active concentration of GABA alone and that these two compounds did not stimulate GTPγ[35S] binding in the absence of GABA to any relevant extent clearly show that they acted as positive modulators, without intrinsic agonistic ...
  http://molpharm.aspetjournals.org/content/60/5/963
*  Chapter 22. Sedative-Hypnotic Drugs | Basic & Clinical Pharmacology, 12e | AccessPharmacy | McGraw-Hill Medical
At her annual physical examination, a 53-year-old middle school teacher complains that she has been experiencing difficulty falling asleep and after falling asleep awakens several times during the night. These episodes occur almost nightly and are having a negative impact on her teaching functions. She has tried various over-the-counter sleep remedies, but they were of little help and she experienced "hangover" effects the next day. Her general health is good, she is not overweight, and she takes no prescription drugs. She drinks one cup of decaffeinated coffee in the morning; however, she drinks as many as six cans per day of diet cola. She drinks a glass of wine with her evening meal but does not like stronger spirits. What other aspects of this patient's history would you like to know? What therapeutic measures are appropriate for this patient? What drug, or drugs (if any), would you prescribe? ...
  http://accesspharmacy.mhmedical.com/content.aspx?bookid=388§ionid=45764244
*  Benzodiazepine | Definition of Benzodiazepine by Merriam-Webster
Define benzodiazepine: any of a group of aromatic lipophilic amines (such as diazepam and chlordiazepoxide) used especially as tranquilizers
  https://www.merriam-webster.com/dictionary/benzodiazepine
*  How Long Does Benzodiazepine Stay in the Body? | eHow
Medical professionals measure the time it takes for medications to be metabolized using the term "half-life." The half-life of a medication is the number of hours it takes for the concentration of the benzodiazepine in the blood to fall to half the dose taken. This number can vary from only two hours (such as with Triazolam) to over 200 hours (such as with Ketazolam). The two most common types of benzodiazepines are Alprazolam (Xanax) and Diazepam (Valium). Xanax takes approximately six to 12 hours to reach its half-life, whereas Valium ranges from 20 to 100 hours.. ...
  http://www.ehow.com/how-does_5407511_long-benzodiazepine-stay-body_.html
*  Plus it
Some studies have concluded that E-S potentiation is likely attributable to I-LTD (Chavez-Noriega et al., 1989; Lu et al., 2003), based in part on their findings that E-S potentiation is absent in slices bathed in GABAA receptor blockers. Although our extracellular recordings initially suggested that 5 Hz stimulation-induced E-S potentiation is disrupted by the GABAA receptor blocker picrotoxin, we noted that facilitation of PS amplitudes and bursting during 5 Hz stimulation was strongly disrupted in disinhibited slices. This suggests that blocking inhibition might inhibit the induction of E-S potentiation by 5 Hz stimulation rather than occlude its expression. Indeed, simply doubling the intensity of presynaptic fiber stimulation during 5 Hz stimulation so that EPSPs elicited postsynaptic bursting rescued E-S potentiation in the presence of picrotoxin. Although not statistically significant, the amount of E-S potentiation induced by strong 5 Hz stimulation in ...
  http://www.jneurosci.org/content/29/36/11203
*  Gamma-Aminobutyric Acid-Induced Potentiation of Cortical Hemiplegia
A novel model of hemiplegia in young and aged rats is described. Osmotic minipumps were used to deliver a chronic (7 days), localized application of gamma-aminobutyric acid (GABA) (100 micrograms/microliter/h), to the somatomotor cortex of unrestrained rats. This resulted in an easily quantifiable, contralateral and reversible motor syndrome in both young and aged animals. In the young group, the motor deficit cleared over 5-day period, while in the aged animals it persisted for at least a 2-week period. Control animals treated with saline-filled minipumps did not develop a long-lasting motor deficit. The GABA-induced facilitation of hemiplegia due to small motor cortex lesions and the age effects on behavioral recovery of function are discussed. Cortical inhibitory mechanisms may play a role in debilitating syndromes such as stroke or post-epileptic paralysis.. ...
  http://knightlab.berkeley.edu/publications/detail/17/
*  Plus it
The in vitro binding constants to brain benzodiazepine receptor are known for a variety of benzodiazepines and also for four other different classes of strongly binding compounds. The binding data for a total of 29 drugs selected from these 5 classes was used to deduce a possible binding site model consisting of 15 site points and only 5 adjustable energy parameters. Even though some of the chemical structures differed radically, it was possible to fit the experimental data with a root mean square deviation of 1.1 kcal/mole. Apparently 5 non-hydrogen atoms in each ligand can occupy corresponding points in the site, and thus constitute a possible benzodiazepine pharmacophore. ...
  http://molpharm.aspetjournals.org/content/22/1/11
*  Anxiety | Page 4 | Welcome to LifeWalk
In a new study, researchers identified a key neurotransmitter in a brain area critical to memory that enables us to suppress unwanted thoughts.. The scientists showed that the ability to inhibit unwanted thoughts relies on the neurotransmitter GABA . GABA is the main inhibitory neurotransmitter in the brain, and its release by one nerve cell can suppress activity in other cells to which it is connected.. The finding helps explain why people who suffer from disorders such as anxiety, post-traumatic stress disorder (PTSD), depression, and schizophrenia often experience persistent intrusive thoughts when these circuits go awry, according to researchers at the University of Cambridge in the U.K.. "Our ability to control our thoughts is fundamental to our well-being," said Professor Michael Anderson from the Medical Research Council Cognition and Brain Sciences Unit at the university. "When this capacity breaks down, it causes some of the most debilitating symptoms of psychiatric ...
  http://lifewalk.com.ng/aggregator/sources/10?page=3
*  Benzodiazepines: Good Practice Guidelines for Clinicians | Department of Health
Benzodiazepines are one of the most widely used prescription medicinal products in the world. Benzodiazepines may be prescribed safely in the short-term and are
  http://health.gov.ie/blog/publications/benzodiazepines-good-practice-guidelines-for-clinicians/
*  flubromazolam Benzodiazepine Class Research Chemical
https://www.officialbenzofury.net/products/Flubromazolam.html Flubromazolam is a brand new Benzodiazepine derivative available to buy @ Offical Benzo Fury. Official Benzo Fury is the first ... Write your own product review ... Flubromazolam - Why is it Such a Popular Research ... - ...
  http://howdoibuyflubromazolamonline.s3-website-ap-southeast-2.amazonaws.com
*  Benzodiazepine analysis using RapidFire Dilute and Shoot Methodology | SelectScience
This video, presented by Lauren E. Frick PhD, introduces a poster highlighting the use of the Agilent RapidFire Dilute and Shoot Methodology for Benzodiazepine analysis. The system is a much quicker process for serial on-line solid phased extractions. It generates high quality data, more than 10 x faster than conventional LC/MS methods. In operation, the entire process time from start to finish is less than 9 seconds per sample which results in a throughput of 400 samples per hour.
  http://www.selectscience.net/SelectScience-TV/Videos/benzodiazepine-analysis-using-rapidfire-dilute-and-shoot-methodology/?VideoID=703
*  KAKEN - Research Projects | The roles of glutamic acid and gamma-aminobutyric acid in the convulsive mechanisms of El mice. ...
Principal Investigator:YOKOI Isao, Project Period (FY):1989 - 1991, Research Category:Grant-in-Aid for General Scientific Research (C), Research Field:Psychiatric science
  https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-01570607/
*  Difference between revisions of "Experimental Anaesthesiology Antkowiak Lab:Poster" - OpenWetWare
Grasshoff C, Schweizer J, Netzhammer N, Antkowiak B, Hentschke H: Thiopental's effects on GABAergic currents in spinal ventral horn networks in vitro: concentration-dependent shifts of impact from phasic to tonic currents, [[Media:2007_poster_cg.pdf , pdf ca. 4,7 MB ...
  https://openwetware.org/wiki/?title=Experimental_Anaesthesiology_Antkowiak_Lab:Poster&diff=570661&oldid=462765
*  What is gabapentin made of - Kgb Answers
What is gabapentin made of The KGB Agent answer: Not Medical Advice: Gabapentin is made up of similar structure to the neurotransmitter GABA but is not believed to act on the same brain receptors.
  http://www.kgbanswers.com/what-is-gabapentin-made-of/11032231