The inhibitory power (Z) of a number of (R)-l-alkyl-2-acylamino phospholipid analogues was determined for three mammalian phospholipases A2 from pig, ox and horse pancreas. All three enzymes display a clear preference for anionic (phosphoglycol) inhibitors over the zwitterionic (phosphocholine) ...

We examined the effects of γ-hydroxy butyrate (GHB) alone and in combination with either ethanol or NCS 382 [(2E)-(5-hydroxy-5,7,8,9-tetrahydro-6H-benzo[a][7]annulen-6-ylidene], a purported antagonist at the GHB receptor. These effects were examined on the responding of rats under a fixed-ratio...

γ-Hydroxybutyrate (GHB) has a complex array of neural actions that include effects on its own high-affinity GHB receptor, the release of neuroactive steroids, and agonist actions at GABAA and GABAB receptors. We previously reported partial overlap in the c-Fos expression patterns produced by GH...

γ-Hydroxybutyric acid (GHB), a naturally occurring metabolite of γ-aminobutyric acid (GABA), has been postulated to act both as a specific agonist of GHB receptors and as a weak GABAB receptor agonist. The racemic compound 6,7,8,9-tetrahydro-5-hydroxy-5H-benzocyclohept-6-ylideneacetic acid (RS...

γ-Hydroxybutyric acid (GHB), a minor metabolite of the inhibitory neurotransmitter GABA, can accumulate to significant concentrations in the heritable disorder of GABA degradation, succinic semialdehyde dehydrogenase (SSADH) deficiency (SSADHD). Moreover, GHB may be employed in therapeutic sett...

We report the in vitro assessment of pharmacotoxicity for the high-affinity GHB receptor ligand, NCS-382, using neuronal stem cells derived from mice with a targeted deletion of the aldehyde dehydrogenase 5a1 gene (succinic semialdehyde dehydrogenase(SSADH)-deficient mice). These animals represe...

3-Arylisoxazoles and 3-aryl-2-isoxazolines are versatile building blocks in organic chemistry. They are components of a wide number of pharmaceutical products and biologically active molecules. This chapter describes developments in the chemistry of these heterocycles, focusing on synthetic meth...

Hydroxyamino analogues of γ-aminobutyric acid (GABA) were synthesized and evaluated for inhibitory activity toward γ-aminobutyric acid aminotransferase (GABA-T). The title compound, 3-(hydroxyamino)propylamine (HPA), showed a potent inhibitory activity. The inhibition is competitive with respe...

Perlite sulfonic acid (Perlite-SO3H (PeSA)) has been synthesized by grafting the sulfonic groups on the perlite surface as naturally and cheap support to produce novel heterogeneous reusable solid acid catalysts. FT-IR, XRD, SEM, TGA, pH analysis and Hammett acidity function were employed to cha...

New series of thiourea derivatives incorporating a hippuric acid moiety have been synthesized through the reaction of 4-hippuric acid isothiocyanate with various nitrogen nucleophiles such as aliphatic amines, aromatic amines, sulfa drugs, aminopyrazoles, phenylhydrazine and hydrazides. The synt...

The benzophenone- and acetophenone-photosensitized E—Z isomerization of benzylidene camphor (BC) and p-trimethylammoniobenzylidene camphor methylsulphate was studied quantitatively. Initial sensitized quantum yields and concentrations of both isomers in the photostationary state were measured i...

UV-filters are increasingly used in cosmetics and in the protection of materials against UV-irradiation. The widespread occurrence of UV-filter residues in aquatic systems has been reported, but still little is known about their environmental effects. Some of these compounds negatively interact ...

The E ⇄ Z photoisomerization of benzylidene camphor and benzylidene tetrahydrofuranone was examined in various solvents. The isomerization quantum yields determined from different methods were found to be independent of the concentration and of the irradiation wavelength. No solvent and oxygen e...

UV filters represent new classes of estrogenic [Environ. Health Perspect. 109 (2001) 239] or antiandrogenic [Toxicol. Sci. 74 (2003) 43] chemicals. We tested 3-benzylidene camphor (3-BC), reported as estrogenic in fish [Pharmacol. Toxicol. 91 (2002) 204], and mammalian systems in comparison to 4...

UV-filters are widely used in many personal care products and cosmetics. Recent studies indicate that some organic UV-filters can accumulate in biota and act as endocrine disruptors, but there are few studies on the occurrence and fate of these compounds in humans. In the present work, a new liq...

A straightforward analytical method for determination of 3-benzylidene camphor (3-BC) in rat adipose tissue, brain, liver, muscle, plasma and testis following topical application was developed and validated. Three exposure levels (60, 180 and 540 mg kg−1 day−1) were tested for 65 days in male Sp...

[4-14C]Estrone was injected into three mature Rhode Island hens. Radioactive steroids and steroid conjugates were recovered from the urine on columns of Amberlite XAD-2 and fractionated on columns of DEAE-Sephadex A-25 in a NaCl gradient. Two minor less polar radioactive fractions (I and II) wer...

The photophysical and photochemical properties of fingerprint reagent - 1,8-diazafluoren-9-one (DFO) - were studied using steady-state, time-resolved spectroscopic techniques and semiempirical quantum-chemical calculations. In order to understand how microenvironment influences the excited-state...

We study a fluid-fluid phase transition of the explicit solvent model represented as a mixture of the restricted primitive model (RPM) of ionic fluid and neutral hard spherocylinders (HSC). To this end, we combine two theoretical approaches, i.e., the scale particle theory (SPT) and the associat...

The solvent resistance performance of organic solvent nanofiltration (OSN) membranes still need to improve for their applications in harsh organic environments. We envisioned that fluorine (F) atoms could enhance the solvent resistance of OSN membranes owing to the high bond energy of C-F bonds....