A method for the convenient synthesis of phosphonothioates, or phosphonothioic acids, is reported. A significant advantage of the method is the alleviation of the need for purification of intermediates, other than washing with water. No chromatography is needed and the only purification step is ...

Dyfonate (O-ethyl S-phenyl ethylphosphonodithioate) is rapidly metabolized in living rats to form polar products which are excreted in the urine and in the feces via the bile. The identified metabolites account for more than 94% and 78% of the administered dose from both the phosphorus- and thio...

When enantiopure tert-butyl(phenyl)phosphine oxide 1 was used as a resolving agent, it showed an acceptable to good chirality-recognition ability for several kinds of racemic carboxylic acids 2. A study on a chirality-recognition mechanism based on X-ray crystallographic analyses of the diastere...

Phenyl phosphonothioic acid-O-ethyl-O-[4-nitrophenyl] ester (EPN) is one of the 10 most frequently used organophosphorus insecticides and caused delayed neurotoxicity in adult chickens and mallards. Small amounts of organophosphorus insecticides placed on birds' eggs are embryotoxic and ter...

Ab initio molecular orbital theory with the 6-31G(d), 6-31+G(d), 6-31G(d,p), and 6-31G(2d) basis sets has been used to calculate the geometry optimized structures and the relative energies (ΔE) of the rotamers of the chair conformers of 3-substituted equatorial tetrahydro-2H-thiopyran-1-oxides ...

We investigated the binding properties of the (R)- and (S)-enantiomers of the muscarinic antagonists trihexyphenidyl, procyclidine, hexahydro-difenidol, p-fluoro-hexahydro-difenidol, hexbutinol, p-fluoro-hexbutinol, and their corresponding methiodides at muscarinic M1, M2, M3 and M4 receptor sub...

P2 membrane receptors for nucleotides represent significant targets for experimental pharmacology and drug research. In earlier publications, we have shown that Reactive Blue 2 (RB 2), one of the most widely used P2-receptor antagonists, displays only moderate affinity and does not discriminate ...

Recent studies have suggested that extrasynaptic GABAA receptors, which contribute tonic conductance, are important targets for general anesthetics. We tested the hypothesis that manipulations designed to alter ambient GABA concentrations (tonic conductance) would affect hypnotic (as indicated b...

We have investigated the role of the α subunit in the modulation of γ-aminobutyric acid type A (GABAA) receptors by the general anesthetic propofol, using whole-cell patch clamp recordings made from distinct stable fibroblast cell lines which expressed only α1β3γ2 or α6β3γ2 GABAA recepto...

BackgroundKetamine has been reported to exert anti-inflammatory effects on macrophages stimulated with lipopolysaccharide (LPS) in vitro and in vivo. Several studies have reported conflicting results regarding the effects of propofol on cytokine production from immune cells. However, there have ...

Propofol (i.v. and i.p.) exhibited anticonvulsant activity in three models of seizure in the mouse, induced by bicuculline, kainic acid and N-methyl-DL-aspartic acid (NMDLA). Morphine, pethidine and fentanyl, which showed a biphasic doseresponse relationship with respect to seizure modulation, a...

Cyclic amino acid esters of propofol were synthesized in an attempt to develop new water-soluble anesthetic agents. Their solubility and stability in aqueous solution, and their ability to release propofol in vitro under physiological conditions were determined. l-Proline (6a) and racemic nipeco...

Etomidate and propofol have clearly distinguishable effects on the central nervous system. However, studies in knock-in mice provided evidence that these agents produce anesthesia via largely overlapping molecular targets, namely GABAA receptors containing β3 subunits. Here the authors address ...

PurposeTo investigate the effect of proparacaine hydrochloride eye drops on emergence agitation after general anaesthesia for paediatric strabismus surgery.

In brainstem motor networks, hypoglossal motoneurons (HMs) play the physiological role of driving tongue contraction, an activity critical for inspiration, phonation, chewing and swallowing. HMs are an early target of neurodegenerative diseases like amyotrophic lateral sclerosis that, in its bul...

Post-operative cerebral edema is a threat for patients performed gliomas resection. Some studies have shown that general anesthesia drugs, such as, propofol had neuroprotective effect. Aquaporin-4 (AQP4) and Aquaporin-9 (AQP9) play an important role in maintaining brain water homeostasis under v...

Although propofol is a widely used intravenous general anaesthetic, many studies report its toxic potential, particularly on the developing central nervous system. We investigated its action on hypoglossal motoneurons (HMs) that control two critical functions in neonates, namely tongue muscle ac...

An investigation of the chemical constituents of Salicornia herbacea has led to the isolation of one new natural product, pentadecyl ferulate (6), together with 11 known compounds, including phytol (1), stearolic acid (2), γ-linolenic acid (3), (3Z,6Z,9Z)-tricosa-3,6,9-triene (4), linoleic acid...

A new coumarin chalcone 3-((2E)-3-(2-hydroxyphenyl) prop-2-enoyl)-4-hydroxy-2(H)-chromen-2-one was synthesized using the Claisen Schmidt reaction by the condensation of 3-acetyl-4-hydroxycoumarin and 2-hydroxybenzaldehyde using a mild organic base. This novel compound was characterized by 1H NMR...

Complexes of Tb(III) with the biscoumarin derivative 3,3′-[(4-hydroxyphenyl)methyl]bis-(4-hydroxy-2H-chromen-2-one) are synthesized by using a solution of tetraethylammonium hydroxide, [(C2H5)4N]OH, in water as deprotonating base. Elemental analysis, IR- and fluorescence spectroscopy are used t...