The effect of the anti-epileptic drug 5,5′-diphenylhydantoin (Dilantin) on Na permeability (PNa) in frog skeletal muscle was studied. Because there is no detectable tetrodotoxin-sensitive Na permeability in resting frog muscle, PNa was induced using the alkaloid ‘neurotoxin’ veratridine. Vera...

Adverse effects of anti-seizure/anti-epileptic medications on bone density have been observed and reported since the early 1960s. Phenytoin and carbamazepine are two commonly prescribed anti-epileptic drugs most frequently associated with osteomalacia including fractures, bone demineralization, ...

AimTo develop a simplified and fully automated synthesis procedure of 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) using PET-MF-2V-IT-I synthesis module.

3′-Deoxy-3′-fluorothymidine (FLT, alovudine®) belongs to the most potent agents inhibiting HIV-1 replication. Its 5′-triphosphate (FLTTP) is a potent inhibitor of HIV-1 reverse transcriptase (HIV RT). Unfortunately, FLT exerts substantial hematologic toxicity both in vitro and in vivo. It was...

Microscale radiosynthesis on a miniaturized device has been reported as a promising tool for positron emission tomography. Here, we studied miscroscale-level radiosynthetic conditions by examining several microscale reactions that affect the radiochemical yield of 3′-deoxy-3′-[18F]fluorothymid...

The use of methyl 5-0-tert-butyldiphenylsilyl-2-deoxy-α , β -D-threo-pentofuranoside, prepared from D-xylose,as a divergent intermediate for the synthesis of 3'-substituted-2',3'-dideoxynucleosides is illustrated by its conversion into 3'-azido-3'-deoxythymidine, 3...

We prepared 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) from 3′-O-nosyl thymidine derivative 3 or its pyrimidine ring N-BOC-protected analogue 5 and optimized [18F]fluorination condition for a high radiochemical yield. The optimal condition for [18F]fluorination with precursor 3 was 30 mg (41...

Imaging the pharmacodynamics of anti-cancer drugs may allow early assessment of anti-cancer effects. Increases in 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT) uptake early after thymidylate synthase inhibition (TS) inhibition, the so-called flare response, is considered to be largely due to an ...

Two human cell lines (A549 and U937) with cytosolic thymidine phosphorylase (TP) activity were used to evaluate the potential of 5′-deoxy-5′-[F-18]fluorothymidine ([F-18]DFT) as a tracer of intracellular TP expression. Cellular metabolism of DFT led to the production of 5-[F-18]fluoro-2,5-dide...

Transport characteristics for uptake and release of dibromosulphthalein (DBSP) by isolated rat liver cells were studied. The rate of uptake is dependent on the extracellular protein concentration and follows Michaelis—Menten kinetics with respect to the unbound substrate concentration; the proc...

Transport of dibromosulphthalein (DBSP) was investigated in the isolated perfused rat liver as a model for hepatic organic anion transport. The results of the study suggest that uptake and biliary excretion of DBSP are carrier-mediated processes, which possibly differ in their sodium dependency....

Opening of the epoxide ring of several arylglycidyl ethers with thiocyanato anion followed by acetylation yielded racemic mixtures of 1-aryloxy-3-thiocyanato-propan-2-yl acetates. A lipase-catalyzed hydrolysis of the acetates resulted in the separation of the enantiomers. The unstable, optically...

The methodology presented provides a quantitative way to characterize investor behavior and price dynamics within a particular asset class and time period. The methodology is applied to a data set consisting of over 250,000 data points of the S&P 100 stocks during 2004-2018. Using a two-way fixe...

The solvent extraction equilibrium of boron extraction has been studied for petroleum ether, kerosene and chloroform solutions of 2-ethyl-1,3-hexanediol (EHD) and 2-chloro-4(1,1,3,3-tetramethylbutyl)-6-methylolphenol (CTMP or 3-chloro-5-(1,1,3,3-tetramethylbutyl)salicyl alcohol), employed both s...

The solvent extraction equilibrium of boron extraction has been studied for petroleum ether solutions of 2-ethyl-1,3-hexanediol (EHD) and 2-chloro-4-(1,1,3,3-tetramethylbutyl)-6-methylol-phenol (CTMP), employed both singly and in admixture. Theoretical considerations are developed to account sem...

The acid-catalysed dehydration of 1,2-diphenyl-4-dimethylaminobutan-2-ol is shown to yield all four possible elimination products. Pure samples of cis and trans 4-dimethylamino-1,2-diphenylbut-1-ene and the corresponding trans (H/Ph) but-2-ene have been isolated and their configurations assigned...

Lewis acid (ZnI2) – promoted Mannich reaction of azetidin-2-one – tethered aldimine 3 with silylenol ether 4 in toluene at –20 °C afforded a diastereomeric mixture of β-amino acid esters 5 and 6 in ratio 65:35. Diastereomers 5 and 6 were chromatographically separated and their crystal struc...

A new synthetic route to (3R,4S)-3-hydroxy-4-phenylazetidin-2-one, an important precursor for the paclitaxel side chain, has been developed using intramolecular cyclization of N-(p-methoxyphenyl) (2S,3R)-2-acetoxy-3-bromo-3-phenylpropionamide which can be easily obtained by catalytic asymmetric ...

A regio- and stereoselective cycloaddition of 6,6-spiroepoxycyclohexa-2,4-dienones with indene leading to benzo-annulated spiroepoxytricyclo[5.2.2.02,6]undec-10-en-9-ones has been described. Manipulation of the oxirane ring in adducts furnished benzotricyclo[5.2.2.02,6]undecanes endowed with a β...

A commercial laccase, Suberase® from Novozymes, catalyses the synthesis of triaminated cyclohexa-2,4-dienones and a methylbenzene-1,2-diol derivative. The primary amine (analine) and the catechol was reacted under mild conditions (40 °C) in a reaction vessel open to air in the presence of Suber...