Loading...
*  Sodium thiopental - Wikipedia
... effects of barbiturates.[25] The GABAA receptor is an inhibitory channel that decreases neuronal activity, and barbiturates ... Selfotel; Glycine site antagonists: 4-Cl-KYN (AV-101). *5,7-DCKA ... GABA receptor modulators. GABAA receptor positive modulators. ... Surprisingly, while GABAA receptor currents are increased by barbiturates (and other general anesthetics), ligand-gated ion ... Main article: Barbiturate. Sodium thiopental is a member of the barbiturate class of drugs, which are relatively non-selective ...
  https://en.wikipedia.org/wiki/Pentothal
*  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
*  Barbiturates
... rather than to act as GABA antagonists, as do certain other convulsants. Clearly, the convulsant barbiturates must possess ... Barbiturate Interactions with g-Aminobutyric Acid (GABA) Postsynaptic inhibition in the brain, is usually mediated by GABA (38 ... These findings led naturally to a focus on interactions of barbiturates with the GABAA receptor. This 'classical' GABA receptor ... the GABAA receptor (5,46), with barbiturates causing an increase in the binding of labeled GABA and benzodiazepines to the ...
  http://www.acnp.org/g4/GN401000173/CH169.html
*  Unit 3 - Sedative-Hypnotic Drugs Flashcards by Annette Liem | Brainscape
synthetic benzodiazepine antagonist used to reverse benzo and pseudo-benzo OD. -no effect on GABA-A receptor function per se ... both are barbiturates. PB: less lipid soluble, slower onset, slow elimination (t 1/2 = 4-5 days), so longer-acting. -used as ... blocks GABA-A Cl- channel directly (non-competitive antagonist) that causes convulsions ... bind to some site on GABA-A receptor complex to potentiate GABA-mediated inhibition. -opens Cl- channel --> hyperpolarize cell ...
  https://www.brainscape.com/flashcards/unit-3-sedative-hypnotic-drugs-2931718/packs/4527857
*  Application # 2017/0319560. PYRAZOLE, TRIAZOLE AND TETRAZOLE OREXIN RECEPTOR ANTAGONISTS - Patents.com
The present invention is directed to pyrazole, triazole and tetrazole compounds which are antagonists of orexin receptors. The ... barbiturates, cyclopyrrolones, GABA agonists, 5HT-2 antagonists including 5HT-2A antagonists and 5HT-2A/2C antagonists, ... antagonists, melatonergic agents, benzodiazepines, barbiturates, 5HT-2 antagonists, and the like, such as: adinazolam, ... protein antagonists, ghrelin receptor antagonists, histamine 3 receptor antagonists or inverse agonists, and neuromedin .orgate ...
  http://patents.com/us-20170319560.html
*  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=
*  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
*  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
*  phenobarbital (CHEBI:8069)
GABA modulator A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor- ... A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl ... GABA modulator A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor- ... GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by ...
  https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8069
*  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
*  diazepam (CHEBI:49575)
GABA modulator A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor- ... a site at which barbiturates act to prolong the duration of channel opening; and a site at which some steroids may act. ... GABA modulator A substance that does not act as agonist or antagonist but does affect the gamma-aminobutyric acid receptor- ... GABA-A receptors appear to have at least three allosteric sites at which modulators act: a site at which benzodiazepines act by ...
  https://www.ebi.ac.uk/chebi/searchId.do?chebiId=49575
*  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
*  Receptors and Centrally Acting Drugs Pharmacokinetics and Drug Metabolism - 1st Edition
Effect of Drugs Classified as α2-Adrenoceptor Agonists and Antagonists on the Electroshock-Induced Seizures in Mice. GABA and ... The Effect Of 2,3-Benzodiazepines on the Benzodiazepine-GABA-Picrotoxin/Barbiturate-Cl Ion Channel Complex. ACTH and Related ... Interaction of Different Compounds, having Atypical Anxiolytic Properties with GABA-Benzodiazepine Receptor Complex. GABA ... GABA Receptors in the Myenteric Plexus from Morphine-Tolerant Guinea-Pigs. The Effect of L-Noradrenaline and Xylazine on the ...
  https://www.elsevier.com/books/receptors-and-centrally-acting-drugs-pharmacokinetics-and-drug-metabolism/vizi/978-0-08-034191-0
*  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/
*  ISONICOTINAMIDE OREXIN RECEPTOR ANTAGONISTS - Patent application
... barbiturates, cyclopyrrolones, GABA agonists, 5HT-2 antagonists including 5HT-2A antagonists and 5HT-2λ/2C antagonists, ... antagonists, melatonergic agents, benzodiazepines, barbiturates, 5HT-2 antagonists, and the like, such as: adinazolam, ... protein antagonists, ghrelin receptor antagonists, histamine 3 receptor antagonists or inverse agonists, and neuromedin U ... agonists and antagonists, melatonergic agents, other orexin antagonists, orexin agonists, prokineticin agonists and antagonists ...
  http://www.patentsencyclopedia.com/app/20110201591
*  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
*  Lec 17 & 18 (Anxiety/Epilepsy & Dopamine/Serotonin) Flashcards by Jaclyn Zois | Brainscape
can give flumezanil, a direct antagonist of GABA-receptor -blocks BZD binding site ... barbiturates propofol (at high concentrations propofol and barbiturates act as direct agonists) alcohol benzodiazepines ... inhibits GABA breakdown/catalysis. 3. increase GABA synthesis 4. blocks GABA repute -prolongs signaling 5. protect GABA-A ... positive allosteric modulation of GABA-A receptor. -bind to a separate site -increase affinity of GABA for its receptor, a LGIC ...
  https://www.brainscape.com/flashcards/lec-17-amp-18-anxiety-epilepsy-amp-dopami-6813581/packs/10761323
*  GABAc Receptors in the Vertebrate Retina by Haohua Qian - Webvision
Since the competitive antagonists are thought to interact with the GABA binding sites on the receptors, these results indicate ... such as benzodiazepines and barbiturates). GABA r subunits are thought to participate in forming GABAc receptors on the ... GABAA Receptor. GABAB Receptor. GABAC Receptor. Category. Ligand-gated Channel. G-protein coupled receptor. Ligand-gated ... 5. GABA (10 mM) induced responses from white perch GABA r subunits expressed in Xenopus oocytes. The duration of GABA ...
  https://webvision.med.utah.edu/book/part-v-phototransduction-in-rods-and-cones/gabac-receptors-in-the-vertebrate-retina/
*  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