N-Formyl-leurosine labeled with 14C in the formyl group was administered to six patients with malignant disease, and the pharmacokinetic behavior of the drug was determined. Chromatographic studies on plasma showed the presence of unchanged drug and 7 metabolites. No metabolites were found in th...
Radio-detoxified endotoxin (Tolerin®), produced by 60Co-γ irradiation of Escherichia coli 089 endotoxin, can protect dogs against the acute cardiotoxic side-effects of formyl-leurosine, a semi-synthetic Vinca derivative with promising antineoplastic potency. Formyl-leurosine induces a rapid dec...
A gas-liquid chromatographic assay has been developed to measure isethionic acid after methylation with diazomethane. The identity of the products of methylation has been confirmed by mass-spectrometry and nuclear magnetic resonance spectroscopy. The method was used to measure isethionic acid in...
Four new zwitterionic butanesulfonic acid buffers that are structurally related to four families of Good buffers were evaluated for use in biological systems. These buffers, with pKa values from 7.6 to 10.7, were compared with a variety of other buffers from the same family and with unrelated bu...
Based on the principle of separation by capillary electrophoresis, three simple molecular structural descriptors, the number of acid groups (NG), number of atoms (NA) and molecular weight (MW) were employed to model the molecular structure–electrophoretic mobility relationship with the general ...
Indeno[2′,1′:5,6]pyrido[2,3-d]pyrimidin-4,6-(5H,11H)dione derivatives were synthesized regioselectively in high yields by a three-component reaction of 1,3-indanedione, aromatic aldehydes and 2,6-diaminopyrimidin-4(3H)-one in the presence of 1,2-dimethyl-N-butanesulfonic acid imidazolium hydro...
Iodide photolysis under UV illumination affords an effective method to produce hydrated electrons (eaq–) in aqueous solution. Therefore, UV/Iodide photolysis can be utilized for the reductive degradation of many recalcitrant pollutants. However, the effect of naturally occurring organic matter ...
Production of biodiesel from sewage sludge lipids was catalysed by six different Brønsted acidic imidazolium and long chain ammonium ionic liquids; both with an alkane sulfonic acid group and with different anions. Among the ionic liquid tested, 4-(3-methylimidazolium) butanesulfonic acid triflu...
In connection with the acquisition of knowledge for an expert system for solid-phase extraction (SPE), a preliminary investigation was made of the kinds of sorbents that can be used for the SPE of small acid analytes. The development of a simultaneous solid-phase extraction of the preservatives ...
An anionic method for preparation of water-soluble block copolymer of 2-isopropenylnaphthalene and methacrylic acid poly(2-IPN-b-MAA), containing pyrene group as a terminal probe, is described. The polymerization process was carried out by an indirect method employing trimethylsilyl methacrylate...
In fluid solution poly(2-isopropenylnaphthalene) (PIPN) forms excimers more readily than any other known polymer. Its fluorescence spectrum in 2-methyl-THF solution at 77 K consists nevertheless of emission from isolated “monomeric” naphthalene chromophores. The delayed luminescence of these g...
2-Isopropenylnaphthalene (2-IPN) can be polymerized anionically at −78°C using n-butyllithium as initiator. The “living end” of this polymer can initiate further polymerization. Thus by the addition of thoroughly purified 1,3-butadiene to the polymerization mixture, diblock copolymers of the ...
2-Isopropenylnaphthalene (2-IPN) and 2-vinylnaphthalene (2-VN) were polymerized in toluene with sec-butyllithium initiator. For 2-IPN, equilibrium monomer concentrations were determined, as well as the enthalpy, entropy and ‘absolute’ ceiling temperature, for its polymerization. Densities of b...
The atypical chemokine receptor, D6, is efficient at sequestering and scavenging inflammatory CC chemokines. The absence of D6 blocks the successful resolution of immune responses in models of inflammation, suggesting that CC-chemokine scavenging by D6 is an important component of the resolution...
IntroductionVesicular monoamine transporters 2 (VMAT2) in the brain serve as transporter for packaging monoamine in vesicles for normal CNS neurotransmission. Several VMAT2 imaging agents, [11C]-(+)-DTBZ, dihydrotetrabenazine and [18F]FP-(+)-DTBZ (9-O-fluoropropyl-(+)-dihydro tetrabenazine, a.k....
A series of amino-2-cyclohexyl ester derivatives were studied for their ion channel blocking and antiarrhythmic actions in the rat and a structure-activity analysis was conducted. The compounds are similar in chemical structure except for ionizable amine groups (pK values 6.1–8.9) and the posit...
Utilisation of acetyl-L-glutamine was studied in growing rats receiving total parenteral nutrition for 15 days. The rats were divided in four groups of 5–8 animals and supplied with an isocaloric nutritional regimen. To all four groups 0.6 g N kg−1 day−1 was given as essential aminoacids. Group...
Glutamine is a metabolite of central importance in nitrogen metabolism of microorganisms and plants. The Chlorella PII signaling protein controls, in a glutamine-dependent manner, the key enzyme of the ornithine/arginine biosynthesis pathway, N-acetyl-L-glutamate kinase (NAGK) that leads to argi...
Afatinib is an irreversible tyrosine kinase receptor inhibitor which was approved lately by USFDA for the treatment of metastatic non-small cell lung cancer (NSCLC). AFT was subjected to stress degradation studies under hydrolytic (acid, base and neutral), oxidative, thermal and photolytic condi...
3-(3,4-Dihydroxyphenyl)-1-n-propylpyrrolidine hydrobromide was synthesized by a six-step reaction sequence and was evaluated, and compared with apomorphine, for central dopaminergic agonist activity. The compound produced behavioral and biochemical changes characteristic of central dopaminergic ...
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