*  Allobarbital - Wikipedia
I. Effects of barbiturates on the convulsive action of GABA-antagonists". Acta Physiologica et Pharmacologica Bulgarica. 13 (3 ... Getova, D.; Georgiev, V. (1987). "GABA-ergic mechanisms in the anticonvulsive activity of newly synthesized barbiturates. ... Allobarbital was never particularly widely used compared to better known barbiturates such as phenobarbital and secobarbital, ... is a barbiturate derivative invented in 1912 by Ernst Preiswerk and Ernst Grether working for CIBA. It was used primarily as an ...
  https://en.wikipedia.org/wiki/Allobarbital
*  Barbiturates Directly Inhibit the Calmodulin/Calcineurin Complex: a Novel Mechanism of Inhibition of Nuclear Factor of...
... the GABAA and GABAB receptor antagonists (+)-bicuculline and CGP 52432 did not diminish the barbiturate-mediated inhibitory ... the naturally occurring agonist GABA was unable to mimic barbiturate-induced repression of NFAT. Second, the GABA antagonists ... GABA Receptors Do Not Mediate the Effect of Barbiturates on NFAT. Most biological effects of barbiturates are mediated through ... Most biological effects of barbiturates are mediated through GABA receptors, and GABA receptor-mediated immunosuppression in T ...
  http://molpharm.aspetjournals.org/content/65/2/350
*  Picrotoxin - Wikipedia
Because it inhibits channels activated by GABA, GABA-enhancing drugs like barbiturates and benzodiazepines can be used as an ... However, due to its antagonist effect on GABA receptors, it has been used as a central nervous system stimulant. It was also ... Other research suggests that the toxin acts instead as a non-competitive antagonist, or inhibitor, for GABA receptors. A study ... Ehrenberger, K.; Benkoe, E.; Felix, D. (1982). "Suppressive Action of Picrotoxin, a GABA Antagonist, on Labyrinthine ...
  https://en.wikipedia.org/wiki/Picrotoxin
*  GABAB Receptor-Mediated Inhibition of Synaptic Transmission in the Hippocampus: Pharmacology and Intracellular Mechanisms |...
GABA) is a major inhibitory neurotransmitter in the central nervous system that affects cellular excitability by opening or ... Soltesz I, Haby N, Leresche N, Crunelli V (1988): The GABAB antagonist phaclofen inhibits the late K+-dependent IPSP in cat and ... especially because of their close association to the benzodiazepine and barbiturate binding sites. More recently, presynaptic ... Huston E, Scott RH, Dolphin AC (1990): A comparison of the effect of calcium channel ligands and GABAB agonists and antagonists ...
  https://link.springer.com/chapter/10.1007/978-1-4684-6825-0_2
*  PATHOGENESIS OF HEPATIC ENCEPHALOPATHY - A ROLE FOR THE BENZODIAZEPINE RECEPTOR? - PDF
A benzodiazepine antagonist does not alter the course of hepatic encephalopathy or neural GABA binding. Metab Brain Dis 2: , ... as different groups found that GABA agonists such as barbiturates, benzodiazepines and muscimol potentiated HE symptoms ( ... 105,106), while the administration of the GABA antagonist bicuculline was found to improve neurophysiological changes and ... changes in GABA neurotransmission could be explained by alterations of either the structure or the level of ligands to the GABA ...
  http://docplayer.net/1208733-Pathogenesis-of-hepatic-encephalopathy-a-role-for-the-benzodiazepine-receptor.html
*  DiVA - Search result
Analogous to benzodiazepine site antagonists, the development of neurosteroid antagonists may help clarify the role of GABA- ... enhance the GABA-mediated Cl- currents acting on a site (or sites) distinct from the GABA, benzodiazepine, barbiturate, and ... 3beta-Hydroxysteroids are also direct, noncompetitive GABA(A) receptor antagonists. 3beta-Hydroxysteroids coapplied with GABA ... GABA-site antagonism and pentobarbital actions do not depend on the α-subunit type in the recombinant rat GABA-A receptor2006In ...
  http://umu.diva-portal.org/smash/resultList.jsf?af=%5B%5D&aq=%5B%5B%7B%22personId%22%3A%22authority-person%3A4528%22%7D%5D%5D&aqe=%5B%5D&aq2=%5B%5B%5D%5D&language=en&query=
*  PPT - Gamma- Amino- Butyric- Acid (GABA) Before 1883 known as a metabolite of plants and microorganisms ...
GABA) Before 1883 known as a metabolite of plants and microorganisms (Basidio-, Streptomycetes) 1883 synthesized 1949 ... antagonist MUSCIMOL pro-convulsive BICUCULLIN (cordyalis lutea = Lerchensporn) (BARBITURATES) Th: former hypnotics ... Gamma- Amino- Butyric- Acid (GABA) Before 1883 known as a metabolite of plants and microorganisms - PowerPoint PPT Presentation ... Gamma- Amino- Butyric- Acid (GABA) Before 1883 known as a metabolite of plants and microorganisms (Basidio-, Streptomycetes) ...
  https://www.slideserve.com/bernad/powerpoint-pr
*  Free Science Flashcards about list of drugs-unit 1
competitive antagonist at GABA(A) receptor -causes seizures. Baclofen (Lioresal). -selective agonist for the GABA(B) receptor - ... Barbiturate (class of drug). -positive allosteric modulators;increase mean open time of GABA(A) channel • Have similar effects ... noncompetitive antagonist at GABA(A) receptor -causes convulsions. Benzodiazepine. -class of drugs that act as CNS depressants ... nonselective 5-HT2A receptor antagonists -used to decrease hypertension. allylglycine. -blocks GABA synthesis -causes ...
  https://www.studystack.com/flashcard-331382
*  Plus it
GABAA-positive modulators, neuroactive steroids, N-methyl-d-aspartate (NMDA) antagonists, and 5-hydroxytryptamine (5-HT)3 ... barbiturates, and benzodiazepines all act as positive modulators at the GABAA receptor, a mechanism that seems to be the basis ... Prince RJ and Simmonds MA (1992) 5β-Pregnan-3β-ol-20-one, a specific antagonist at the neurosteroid site of the GABAA receptor ... 4A), inactive at GABAA receptors (Purdy et al., 1990; Lambert et al., 1995), and both can act as competitive antagonists of ...
  http://jpet.aspetjournals.org/content/314/2/675
*  pentobarbital (CHEBI:7983)
... has role GABAA receptor agonist (CHEBI:91016) pentobarbital (CHEBI:7983) is a barbiturates (CHEBI: ... GABA modulator A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor- ... GABA modulator A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor- ... A GABA receptor agonist specific for GABA. A. receptors, ligand-gated ion channels (also known as ionotropic receptors). ...
  http://www.ebi.ac.uk/chebi/searchId.do?chebiId=7983
*  GABAA receptor - Wikipedia
Orthosteric agonists and antagonists: bind to the main receptor site (the site where GABA normally binds, also referred to as ... The binding site for benzodiazepines is distinct from the binding site for barbiturates and GABA on the GABAA receptor, and ... Antagonists, though they have no effect on their own, compete with GABA for binding and thereby inhibit its action, resulting ... GABA receptors A review of GABA and the receptors to which it binds. Tocris Cookson LTD. Enz R, Cutting GR (1998). "Molecular ...
  https://en.wikipedia.org/wiki/GABAA_receptor
*  Learn: Step 1 - Neuro 4 (by denniskwinn) - Memorize.com - Remember and Understand
Treat overdose w/flumazenil (competitive antagonist at GABA benzodiazepenic receptor). Anesthetics general principles. 1. CNS ... Barbiturates. Phenobarbitol, pentobarbital, thiopental, secobarbital. Barbiturates mechanism. Facilitate GABAa action by ↑ ... 1. Disease causes ↑ dopamine, ↓ GABA+Ach. 2. Reserpine+tetrabenazine - amine depleting 3. Haloperidol - dopamine R antagonist. ... Barbiturates IV anesthetics. Thiopental - high potency, high lipid solubility, rapid entry into brain. Used for induction of ...
  http://memorize.com/step-1-neuro-4/denniskwinn
*  Chronotolerance study of the antiepileptic drug valproic acid in mice
... inhibition of GABA Transaminobutyratre (GABA-T), increased GABA synthesis and decreased turnover [30]. Moreover, VPA attenuates ... Naloxone, a morphine antagonist, has been demonstrated to antagonize also the central depressant effect induced by VPA and that ... In addition to producing sedation and hypnosis, the central inhibitory drugs such as barbiturates are generally known to affect ... GABA) by potentiating the GABA inhibitory activity through several mechanisms including inhibition of GABA degradation, ...
  https://www.jcircadianrhythms.com/articles/10.1186/1740-3391-10-3/
*  Human Metabolome Database: Showing metabocard for Allopregnanolone (HMDB0001449)
However, in pubescent teenagers THP actually becomes a GABA receptor antagonist. GABA (gamma-aminobutyric acid) is the primary ... Allopregnanolone is a neuroactive metabolite of progesterone and a barbiturate-like modulator of central gamma-aminobutyric ... In adults and pre-pubescent chlidren THP normally helps soothe the activity of brain cells by binding to GABA receptors that ... inhibitory neurotransmitter in the brain with most sedatives (tranquilizers, anesthetics and alcohol) acting on the GABA ...
  http://www.hmdb.ca/metabolites/HMDB01449
*  Plus it
... a GABAAreceptor antagonist (Fig. 4 C), but they persisted, although they became slower and less regular, in the presence of 120 ... 5 A). We also examined the effect of methohexital, an ultrashort-lasting barbiturate anesthetic, on the Cs+-induced ... Glutamate receptor antagonists and the adenosine receptor antagonist 8-cyclopentyl-1,3-dipropylxanthin (DCPCX) were obtained ... a GABAB receptor antagonist (n = 5, CA1 neurons). In CA1 neurons recorded in the current-clamp mode, the Cs+-induced rhythmic ...
  http://www.jneurosci.org/content/18/22/9256
*  Psychoactive drug - Wikipedia
For example, propofol is a GABA agonist, and ketamine is an NMDA receptor antagonist. Psychoactive drugs are often prescribed ... Commonly used psychoactive drugs and groups: Anxiolytics Example: benzodiazepines, barbiturates Empathogen-entactogens Example ... Harrison NL, Simmonds MA; Simmonds (1985). "Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat ... Li X, Pearce RA; Pearce (2000). "Effects of halothane on GABA(A) receptor kinetics: evidence for slowed agonist unbinding". The ...
  https://en.wikipedia.org/wiki/Psychoactive_drug
*  FA Pharm: ANS, Neuro, Analgesics Flashcards - Cram.com
Barbiturates: how do barbiturates facilitate GABA-A action increase duration of Cl channel opening which decreases neuron ... Regenerates active cholinesterase, chemical antagonist, used to treat organophosphate exposure. It acan be used as an antidote ... Barbiturates: My friend Barb was very anxious so her doctor gave her barbiturates to increase the duration of the time she ... Barbiturates: what happens if you give barbiturates to a patient in alcohol-induced coma or DT's ...
  http://www.cram.com/flashcards/fa-pharm-ans-neuro-analgesics-360707
*  PSYC Call for Commentators: BIOCHEMICAL BASIS OF COMA (969 lines)
This effect still occurs in the presence of GABA receptor antagonists. The authors note that the K+ mechanism is ubiquitous in ... Gases such as halothane and nitrous oxide might produce technical difficulties but agents such as anaesthetic barbiturates, ... General anaesthetics are mainly GABA agonists but some (such as ketamine) are glutamate antagonists. They also affect other ... It modulates the action of GABA on the GABA receptor, but has no action by itself on this receptor (Dzoljic & van Duijn, 1998 ...
  http://www.bio.net/bionet/mm/neur-sci/1999-September/040643.html
*  Basis of the Gabamimetic Profile of Ethanol
GABAA receptors (GABAAR) have long been implicated in the intoxicating actions of ethanol because GABAAR agonistic barbiturates ... GABA antagonist and benzodiazepine partial inverse agonist reduce motivated responding for ethanol. Alcohol Clin Exp Res. 1993; ... unlike BZDs and barbiturates, ethanol does not appear to act directly on most other GABAA receptor subtypes to enhance GABA ... these findings suggested that ethanol influenced the function of GABA on GABAA receptors. In accord with this conclusion, GABAA ...
  http://pubmedcentralcanada.ca/pmcc/articles/PMC2958095/?lang=en-ca
*  GABAA receptor positive allosteric modulator - Wikipedia
GABA agonist GABA antagonist GABA receptor López-Muñoz F, Ucha-Udabe R, Alamo C (Dec 2005). "The history of barbiturates a ... GABA ergic hypothesis for depression has been proposed. This hypothesis places the GABA system in a central role in the ... Alcohols Barbiturates Benzodiazepines Nonbenzodiazepines (Zaleplon, Zolpidem, Zopiclone) Barbiturates' precise action sites ... "Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor". Science. 232 (4753): 1004-7. doi:10.1126/ ...
  https://en.wikipedia.org/wiki/GABAA_receptor_positive_allosteric_modulator
*  Insect GABA Receptors: Splicing, Editing, and Targeting by Antiparasitics and Insecticides | Molecular Pharmacology
... current amplitude histograms for GABA and GABA with the convulsant antagonist BIDN show that the presence of BIDN leads to a ... RDL Mimics the Barbiturate and Steroid Insensitivity of Native Insect GABA Receptors. GABARs of insects are only weakly ... to yield receptors with properties of both GABAA and GABAC subtypes. Furthermore, GABAA and GABAB receptors, which differ ... The GABAA γ2S subunit also forms a complex with both GABABR1 and GABABR2 subunits to allow agonist-induced receptor ...
  http://molpharm.aspetjournals.org/content/68/4/942
*  Plus it
1989) Barbiturate regulation of kinetic properties of the GABAA receptor channel of mouse spinal neurones in culture. J Physiol ... Pentobarbital prolongs the open time of GABA-activated chloride channels (Nicoll et al., 1975; MacDonald et al., 1989), whereas ... ketamine is a noncompetitive NMDA receptor antagonist (Franks and Lieb, 1994) that also reduces AMPA-mediated depolarization ( ... The barbiturate-ketamine anesthetic regimen in this study was chosen as representative of previous investigations in auditory ...
  http://www.jneurosci.org/content/27/23/6091
*  Textbook of Psychiatry/Psychopharmacology - Wikibooks, open books for an open world
... can increase chloride influx into neurons even when GABA is not present. Chloral hydrate, a weak barbiturate, is still ... It is similar to FGAs in that it is a potent D2 receptor antagonist, but like many other SGAs, it is also a post-synaptic ... Benzodiazepines bind to one type of GABA receptor (GABAA) thereby increasing the receptor's affinity for GABA. Increased GABA ... Barbiturates[edit]. Developed in the 1940's and 50's, barbiturates are now rarely used for the treatment of anxiety due to a ...
  https://en.wikibooks.org/wiki/Textbook_of_Psychiatry/Psychopharmacology
*  Physical dependence - Wikipedia
... nor opioid antagonists or inverse agonists, such as naltrexone (a universal opioid inverse agonist) All[citation needed] GABA ... Sedative hypnotic drugs such as alcohol, benzodiazepines, and barbiturates are the only commonly available substances that can ... Lazarova M, Petkova B, Staneva-Stoycheva D (December 1999). "Effects of the calcium antagonists verapamil and nitrendipine on ... nicotine withdrawal) gabapentin (Neurontin) and pregabalin (Lyrica), calcium channel modifiers that affect GABA antiepileptic ...
  https://en.wikipedia.org/wiki/Physical_dependence
*  Plus it
... a GABA receptor antagonist, blocks the effect of persistent inhibition in ICC (Burger and Pollak, 2001; Pecka et al., 2007). ... under barbiturate anesthesia, which dramatically alters the extent and time course of inhibition in the ICC (Kuwada et al., ... 1989; Tollin et al., 2004; Song et al., 2011; Chung et al., 2014). Consistent with the effects of barbiturate anesthesia, very ... in a study of LSO versus IC ILD sensitivity in bat wherein animals were allowed to recover from barbiturate anesthesia before ...
  http://www.jneurosci.org/content/36/38/9908