The crystal structure of seratrodast (AA-2414), a potent thromboxane A2 (TXA2) receptor antagonist, served as starting point to docking studies with the modeled human TXA2 receptor. This structural approach provides rational basis for the design of new antagonists within the aryl sulfonamide family.

The development of isothermal microcalorimetry to a study of the kinetic and thermodynamics of polymorphic transitions in seratrodast ((±)-7-(3,5,6-trimethyl-1,4-benzoquinon-2-yl)-7-phenylheptanoic acid) Form II is reported. Sieved samples of Form II were allowed to convert to Form I, in a reac...

Photodegradation of seratrodast ([±]-7-(3,5,6-trimethyl-1,4-benzoquinone-2-yl)-7-phenyl-heptanoic acid, SD), a p-benzoquinone anti-asthmatic drug, has been investigated in different solutions. HPLC analysis showed that SD was degradated under UV irradiation at 254 nm to afford three major produ...

A high-performance liquid chromatographic (HPLC) method was developed for the simultaneous determination of seratrodast, a new antiasthmatic drug, and its metabolites (M-I to M-III) in human serum and urine. The method for serum and urine with and without enzymatic hydrolysis using β-glucuronid...

A variety of 2-oxoamides and related amides based on natural and non-natural amino acids were synthesized. Their activity on two human intracellular phospholipases (GIVA cPLA2 and GVIA iPLA2) and one human secretory phospholipase (GV sPLA2) was evaluated. We show that an amide based on (R)-γ-no...

Insulin-like growth factor II (IGF-II) is a polypeptide growth factor thought to be involved in fetal tissue development. We previously showed an increased expression of IGF-II mRNA in human primary liver cancer. The present investigation was undertaken to characterize the overexpressed IGF-II t...

Amino acid (AA) transport systems A and L, which transfer preferentially small neutral AA (SNAA) and large neutral AA (LNAA), respectively, were studied in the isolated soleus muscle with the specific models, 2-(methylamino)isobutyrate (MeAIB) and 2-aminobicyclo[2,2,1]heptane-2-carboxylate (BCH)...

We recently described the purification and cloning of extracellular signal-regulated kinase 1 (ERK1), which appears to play a pivotal role in converting tyrosine phosphorylation into the serine/threonine phosphorylations that regulate downstream events. We now describe cloning and characterizati...

IDDM is known to be associated with genes of HLA complex, particularly alleles of HLA-DQ. The 40-kb TAP gene complex is located approximately 150 kb centromeric to the DQB1 locus. The TAP1-TAP2 protein heterodimer is required for normal expression levels of class I molecules on the surface of ce...

Insulin, rapidly and independently of new protein synthesis, stimulates glucose transport in sensitive target tissues. A cDNA has been cloned from a skeletal muscle library that encodes a novel glucose transporter protein exhibiting the following properties of an insulin-regulated hexose carrier...

The purpose of the present investigation was to compare and evaluate the plasma insulin change, the thermogenic response and the substrate utilization in response to a small(125g) and a large(250g) beef steak and cod fillet. Plasma glucose(mmol/L) which was 4,49 ± 0,2 for the small and 4,34 ± ...

(2S,3R,4S)-4-Hydroxyisoleucine, found in fenugreek, is an insulin secretagogue molecule. Non-natural analogues of (2S,3R,4R)- and (2R,3S,4S)-4-hydroxyisoleucine were efficiently prepared by 1,3-dipolar cycloaddition reactions of chiral nitrones derived from either (−)- or (+)-menthone to alkenes...

Twelve 1-phenyl-, 1-thiocarbamoyl- and 1-N-substituted thiocarbamoyl-3-(2-furyl)-5-phenyl/(2-furyl)-2-pyrazoline derivatives were synthesized. The chemical structures of the compounds were proved by IR, 1H NMR, Mass spectrometric data and microanalyses. The antidepressant activities of the compo...

4-(2-Furyl) benzenamine (FBA), was successfully synthesized by a simple method including substitution of furan on p-nitroaniline followed by reduction of nitro group. Structure of the synthesized monomer was verified using IR, 1H NMR and GC–MS techniques. Corresponding poly(4-(2-furyl) benzenam...

Selective adenosine receptor modulators are potential tools for numerous therapeutic applications, including cardiovascular, inflammatory, and neurodegenerative diseases. In this work, the synthesis and biological evaluation at the four human adenosine receptor subtypes of a series of 9-substitu...

AimsEthanol is known to induce NO release and coronary vasorelaxation. Evidence suggests that K+ channels, especially a Ca2+-activated K+ channel (KCa), may regulate endothelial NO production. We aimed to investigate the ethanol effect on K+ currents in human coronary artery endothelial cells (H...

3-(2-Furyl)biphenyls 2a–d were prepared by the rearrangement of 4-(2-furyl)-1,2-dimethyl-5-nitro-6-phenylpyridinium salts under the action of an alkali solution in aqueous ethanol.

1-(2-Furyl)ethanol 1 was resolved by irreversible transesterification with vinyl acetate using Lipozyme IM or Porcine Pancreas Lipase (PPL) in an organic solvent. (S)-alcohol (99% e.e.) was obtained in 80–85% yield using Lipozyme IM in carbon tetrachloride while (R)-1-(2-furyl)ethyl acetate (96...

The present study was designed to determine the possible significance of a therapeutic dose (0.2 mg) of AO-128 on carbohydrate absorption by measuring the breath hydrogen concentration, which is an index of the amount of unabsorbed carbohydrate in the large intestine. Post-prandial hyperglycemia...

Garcinia mangostana L. (Mangosteen) has been used to treat various pathological conditions, including inflammation and urinary tract infections. Here, we observed that garcinone D, a natural xanthone from mangosteen, promoted the proliferation of C17.2 neural progenitor cells and also resulted i...