GABA Modulators

Publication Title: 
Journal of Ethnopharmacology

Rubus brasiliensis hexanic fraction induced anxiolysis in rodents, which was reversed by flumazenil, a specific GABA(A)-benzodiazepine receptor antagonist (Nogueira et al., 1998a,b). Then, we investigated if this hexanic fraction was able to induce hypnotic, anticonvulsant and muscle relaxant effects, and the involvement of GABA(A)-system. The hexanic fraction (50, 100, 150 and 300 mg/kg, vo) was administered to male Swiss mice, 30 min before the tests.

Author(s): 
Nogueira, E.
Vassilieff, V. S.
Publication Title: 
Journal of Clinical Anesthesia

STUDY OBJECTIVE: To evaluate the effect of a small dose of midazolam (10 microg kg(-1)) on induction and emergence during short-term propofol anesthesia and to investigate the effects of subsequent administration of flumazenil. DESIGN: Double-blinded, prospective, randomized study. SETTING: Operating room of a medical college hospital. PATIENTS: 30 male ASA physical status I and II patients (ages 51 to 75) scheduled for minor surgery under spinal anesthesia.

Author(s): 
Adachi, Y. U.
Watanabe, K.
Higuchi, H.
Satoh, T.
Publication Title: 
Acta Anaesthesiologica Scandinavica

BACKGROUND: Flumazenil is a specific benzodiazepine agonist, which is reported to have a partial benzodiazepine agonist-like effect at a high dose. This study investigated the effects of flumazenil and midazolam on the hypnotic dose of propofol and thiopental in ddY mice, using a behavioral model. METHODS: Mice were given either propofol or thiopental intravenously to induce hypnosis, which was defined as a loss of the righting reflex.

Author(s): 
Adachi, Y. U.
Watanabe, K.
Higuchi, H.
Satoh, T.
Publication Title: 
Phytomedicine: International Journal of Phytotherapy and Phytopharmacology

The anticonvulsant effects of thymoquinone, the major constituent of Nigella sativa seeds, were investigated using pentylenetetrazole (PTZ)- and maximal electroshock (MES)-induced seizure models. We also studied the effect of thymoquinone on pentobarbital-induced hypnosis, locomotor activity, and motor coordination. In PTZ-induced seizure, the intraperitoneally injection of thymoquinone with doses of 40 and 80 mg/kg, prolonged the onset of seizures and reduced the duration of myoclonic seizures.

Author(s): 
Hosseinzadeh, H.
Parvardeh, S.
Publication Title: 
Indian Journal of Experimental Biology

Pentobarbitone-induced hypnosis test was used as an animal model to explore the role of BR-16A, a polyherbal formulation in sleep. Pentobarbitone produces quick sleep latency (onset) and prolongation of total sleep time (duration). Sleep latency and total sleep time were used as a parameters for the evaluation. BR-16A potentiated the effect of triazolam (0.1 mg/kg, ip) and alprazolam (0.25 mg/kg, ip). Melatonin (5.0 mg/kg, ip) and zolpidem (0.5 mg/kg, ip) did not produce any significant effect on sleep parameters.

Author(s): 
Kumar, Anil
Kulkarni, S. K.
Publication Title: 
European Journal of Pharmacology

Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate (TG41) enhanced the binding both of gamma-aminobutyric acid (GABA) and of flunitrazepam to rat cerebral cortical membranes. Electrophysiological recordings from Xenopus oocytes expressing various recombinant GABA(A) receptor subtypes revealed that TG41 enhanced the function of all receptor subunit combinations tested. The potency of TG41 at receptors containing alpha1, beta2, and gamma2L subunits was greater than that of alphaxalone, etomidate, propofol, or pentobarbital.

Author(s): 
Mascia, Maria Paola
Asproni, Battistina
Busonero, Fabio
Talani, Giuseppe
Maciocco, Elisabetta
Pau, Amedeo
Cerri, Riccardo
Sanna, Enrico
Biggio, Giovanni
Publication Title: 
Der Anaesthesist

Clinically used anesthetics show amnestic, sedative, hypnotic and immobilizing properties. On a molecular level these drugs affect several receptors in the cell membrane of neurons. By using genetically engineered mice a linkage can now be made between actions on certain receptors and clinically desired and undesired effects. Experiments show that a certain GABA(A) receptor subtype mediates hypnosis and immobility, whereas another subtype is involved in side-effects like sedation and hypothermia.

Author(s): 
Drexler, B.
Grasshoff, C.
Rudolph, U.
Unertl, K.
Antkowiak, B.
Publication Title: 
Alcoholism, Clinical and Experimental Research

BACKGROUND: Emerging evidence implicates metabotropic glutamate receptor (mGluR) function in the neurobiological effects of ethanol. The recent development of subtype specific mGluR antagonists has made it possible to examine the roles of specific mGluRs in biochemical and behavioral responses to ethanol. The purpose of the present study was to determine if mGluRs modulate the acute sedative-hypnotic properties of ethanol in mice.

Author(s): 
Sharko, Amanda C.
Hodge, Clyde W.
Publication Title: 
Anesthesia and Analgesia

BACKGROUND: Benzodiazepines are widely used in clinical anesthesia as premedication, but also to induce general anesthesia. Recent in vitro studies suggest that ?-aminobutyric acid type A receptors, harboring a classical high-affinity benzodiazepine binding site, possess another "nonclassical" binding site for benzodiazepines. At present, it is unclear if, and to what extent, this novel nonclassical binding site is of relevance for the actions of benzodiazepines in the central nervous system.

Author(s): 
Drexler, Berthold
Zinser, Stefan
Hentschke, Harald
Antkowiak, Bernd
Publication Title: 
Phytomedicine: International Journal of Phytotherapy and Phytopharmacology

This study investigated the hypnotic, anti-convulsant and anxiolytic effects of 1-nitro-2-phenylethane (BPNE) obtained from the oil of Dennettia tripetala G. Baker (Annonaceae) and established its mechanism of action. The essential oil (EO) from the leaf, fruit and seed was obtained by hydrodistillation, followed by isolation of BPNE purified to 99.2% by accelerated gradient chromatography on silica, and identified by NMR and GC-MS. The pure BPNE and EO of the dried seed (93.6%) were comparatively evaluated for hypnotic, anticonvulsant and anxiolytic effects in mice.

Author(s): 
Oyemitan, Idris Ajayi
Elusiyan, Christianah Abimbola
Akanmu, Moses Atanda
Olugbade, Tiwalade Adewale

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