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Although morel mushrooms are widely used as tasty ingredients in savory dishes, knowledge of the key compounds evoking their attractive taste is still very fragmentary. In the present study, taste activity-guided fractionation of an aqueous morel extract by means of the recently developed taste
Using immunohistochemistry and optical densitometry, somatostatin (SOM), calcitonin gene-related peptide (CGRP), and gamma-aminobutyric acid (GABA) were investigated in the lumbosacral spinal cord of the frog Rana catesbeiana after sciatic nerve transection. In control animals, the densest network
Gamma-aminobutyric acid type A (GABA(A) )receptors are targets for allosteric modulation by general anesthetics. Mutation of Ser270 within the second transmembrane domain of the GABA(A) receptor alpha subunit can ablate the modulation of the receptor by the anesthetic ether isoflurane. To
Background
The γ-aminobutyric acid (GABA) transporter GAT1 is involved in GABA transport across the biological membrane in and out of the synaptic cleft. The efficiency of this Na
+ coupled GABA transport is regulated by an electrochemical gradient, which is directed
In burning mouth patients, analgesia after oral administration of clonazepam may result from modulation of peripheral γ-aminobutyric acid (GABA) receptors.
The effect of oral administration of test solutions (water, 0.5 mol/L or 0.05 mol/L GABA, 1% lidocaine) was investigated for the amelioration of
BACKGROUND
Most anesthetics, particularly intravenous agents such as propofol and etomidate, enhance the actions of the neurotransmitter γ-aminobutyric acid (GABA) at the GABA type A receptor. However, there is no agreement as where anesthetics bind to the receptor. A novel approach would be to
BACKGROUND
Anesthetics mediate portions of their activity via modulation of the γ-aminobutyric acid receptor (GABAaR). Although its molecular structure remains unknown, significant progress has been made toward understanding its interactions with anesthetics via molecular modeling.
METHODS
The
For the first time, the potential immunomodulators prostaglandin E2 and γ-aminobutyric acid (GABA) have been revealed in the plerocercoid Diphyllobothrium dendriticum, which is a parasite in the tissues and abdominal cavity of the Baikal omul Coregonus migratorius. The localization of
This study investigated the presence of the putative peripheral neuromodulators Gamma-aminobutyric Acid (GABA) and Bombesin/Gastrin-Releasing Peptide (BN/GRP) in the human tooth pulp. Caries free and asymptomatic carious teeth were processed for paraffin embedding and sectioned at six microns. From
Alcohols in the homologous series of n-alcohols increase in central nervous system depressant potency with increasing chain length until a "cutoff" is reached, after which further increases in molecular size no longer increase alcohol potency. A similar phenomenon has been observed in the regulation
Propofol, an intravenous anesthetic, is a positive modulator of the GABAA receptor, but the mechanistic details, including the relevant binding sites and alternative targets, remain disputed. Here we undertook an in-depth study of alkylphenol-based anesthetic binding to synaptic membranes. We
The experiments were carried out on rabbits with ventricular arrhythmias (VA) induced by hypothalamic electric stimulation. The effects of GABA or diazepam (Dz) and picrotoxin on VA were observed. After GABA 0.25, 0.5, 1 mg/rabbit were injected into cerebral ventricle (icv) or cisterna magna (icm),
A series of 4-(piperidin-4-yl)-1-hydroxypyrazole (4-PHP) 3- or 5-imidazolyl substituted analogues have been designed, synthesized, and characterized pharmacologically. All analogues showed binding affinities in the low micro- to low nanomolar range at native rat GABAA receptors and were found to be
γ-aminobutyric acid-type A (GABAA) receptors mediate fast synaptic inhibition in the central nervous system of mammals. They are modulated via several sites by numerous compounds, which include GABA, benzodiazepines, ethanol, neurosteroids and anaesthetics among others. Due to their potential as
A series of bioisosteric N1- and N2 -substituted 5-(piperidin-4-yl)-3-hydroxypyrazole analogues of the partial GABAA R agonists 4-PIOL and 4-PHP have been designed, synthesized, and characterized pharmacologically. The unsubstituted 3-hydroxypyrazole analogue of 4-PIOL (2 a; IC50 ∼300 μM) is a weak