The effect of 1-{1-[4-(3-acetylaminopropoxy)benzoyl]-4-piperidyl-3,4-dihydro-2(1H)-quinolinone} (OPC-21268) on vascular action of arginine vasopressin (AVP) was examined in cultured rat vascular smooth muscle cells (VSMC) by the measurement of cytosolic free calcium concentration ([Ca2+]i) and t...

To study the role of vasopressin (VP) in essential hypertension, we examined plasma levels of VP and blood pressure (BP) response to an orally active V1 receptor antagonist, OPC-21268, in hypertensive patients on diets with different sodium contents. Plasma VP was determined in 12 normotensive s...

N-Acetylhemiaminal metabolites of 1-{1-[4-(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone (OPC-21268) (1), which is a new vasopressin V1 receptor antagonist were synthesized by oxidative decarboxylation of the corresponding α - amino acid derivatives with lead tetraace...

OPC-21268 (1-[-1-[4-(3-acetylaminopropoxy)benzoyl]-piperidyl]-3,4-dihydro-2(1H)-quinolinone), a non-peptide vasopressin V1 receptor antagonist, inhibited oxytocin- and vasopressin-induced contractions of myometrial strips from rats and from full-term pregnant women. Administered intravenously in...

A non-peptide, vasopressin V1a receptor-selective antagonist, OPC-21268, exhibited a markedly higher affinity for the rat V1a receptor (Ki=380 nM) than for the human V1a receptor (Ki=140 μM). To delineate the region responsible for the high affinity binding of OPC-21268 for the rat V1a receptor...

To discover potential inhibitors of the quorum sensing (QS) system, a library of microbial culture extracts was screened with Chromobacterium violaceum CV026 strain. The culture extract of Streptomyces xanthocidicus KPP01532 contained quorum-sensing inhibitors (QSIs) of the CV026 strain. The act...

Publisher SummaryThis chapter focuses on the low-molecular weight carbohydrates that can be formally considered as the oxidation products of mono- or oligo-saccharides in which an aldehyde group and/or one or more hydroxyl groups have been oxidized to carbonyl and/or carboxyl groups. Some acids ...

Di-O-benzylidene derivatives of pentonic acids may be readily prepared by oxidation of the di-O-benzylidene-aldehydo-pentoses with chromium trioxide in N,N-dimethylformamide or by saponification of the corresponding methyl esters. Treatment of ammonium D-xylonate with benzaldehyde and hydrochlor...

In this study, biomass-hydrolysate was used for enhancing the bioreduction of ethyl 4-chloro-3-oxobutanoate (COBE). Firstly, dilute alkalic salt pretreatment was attempted to pretreat bamboo shoot shell (BSS). It was found that enzymatic in situ hydrolysis of 20–50 g/L BSS pretreated with dilut...

The cis-1-chloro-2,3,3,3- tetrafluoropropene (R-1224yd(Z)) is a new low global warming potential promising working fluid in high temperature heat pumps and organic Rankine cycle. In this study, the thermal conductivity was measured in the temperatures from 317 to 416 K with pressures from 1.0 to...

Equilibrium solubility of 7-chloro-quinaldine, 7-chloro-quinaldine L-tartrate or 7-chloro-quinaldine p-nitrophthalate in methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol and acetone was measured by static gravimetric method at temperatures from 283.15 K to 323.15 K under p = 101...

Fluorescent labeling is a widely-used approach in the study of intracellular processes. This method is becoming increasingly popular for studying small bioactive molecules of natural origin; it allows us to estimate the vital intracellular changes which occur under their influence. We propose a ...

5′-Fluoro-5′-deoxyinosine (5′-FDI) is identified as an adventitious side product that accumulates in cell free incubations of SAM and fluoride ion in Streptomyces cattleya. 5′-FDI was identified by a combination of isotopic labelling studies and co-synthesis studies as well as enzymatic degr...

The C-scorpionate iron(II) complexes [FeCl2{κ3-HC(pz)3}] (1) (pz = pyrazol-1-yl), Li[FeCl2{κ3-SO3C(pz)3}] (2) and the new [FeCl2{κ3-HOCH2C(pz)3}] (3) act as catalysts for the hydrocarboxylation of cyclohexane (with CO and H2O) to cyclohexanecarboxylic acid in a remarkable yield (up to 60%) an...

The lower bioavailability of iron from the diet has led to iron deficiency and several ill-effects on health. The objective of this study was to assess the bioavailability of iron from spray dried whey protein concentrate-iron (WPC-Fe) complex in weaning and anaemic rats. Blood hemoglobin level,...

The main aim of this work was to study the mechanisms of interaction between iron(II) ions and humic acids as a function of pH, iron concentration and various humic acids chemical properties, including the degree of humification, elemental composition, aromaticity and content of acidic functiona...

The caffeine absorption/desorption properties of cross-linked membranes prepared from poly(ethylene oxide-co-epichlorohydrin) P(EO/EP) copolymers were determined in order to study the possibility to apply these elastomeric membranes as reservoir in transdermal therapeutic systems. The transport ...

Targeting antigen combined with adjuvants to hepatic antigen-presenting cells (APCs) is essential for the induction of intrahepatic T cellular immunity controlling and resolving viral infections of the liver. Intravenous injection of antigen-loaded nanoparticles is a promising approach for the d...

A bladder instillation of EO-9 (EOquin™) is currently used in phase II clinical trials for the treatment of superficial bladder cancer. Three alternative formulations were developed to improve its pharmaceutical properties and clinical acceptability. Freeze-dried products composed of EO-9, 2-hyd...

Using power distance (PD) and individualism (ID), this study examines the impact of cross-functional cooperation and competition on the EO–performance link in different cultural settings. This study is the first to take departments’ cooperative and competitive behavior into account. A study of...