mefloquine (mfq), as a racemic mixture is used for the prophylaxis and treatment of malaria. stereoselective pharmacodynamic and pharmacokinetic differences have been observed for mfq. in the present study, the human blood was spiked with racemic mfq. the concentration of mfq enantiomers in various blood fractions including packed erythrocyte layer, platelet rich plasma and platelet poor plasma...

BACKGROUND Isoflurane in clinical use is a racemate of S- and R-isoflurane. Previous studies have demonstrated that the effects of S-isoflurane on relevant anesthetic targets might be modestly stronger (less than 2-fold) than R-isoflurane. The X-ray crystallographic structure of the immunological target, leukocyte function-associated antigen-1 (LFA-1) with racemic isoflurane suggested that only...

Carvedilol is administered as a racemic mixture of the R(+)- and S(-)-enantiomers, although it was demonstrated that the two enantiomers exhibit different pharmacological effects and stereoselective pharmacokinetics. The aim of this study was the evaluation of several native and derivatized cyclodextrines as chiral selectors for the separation of carvedilol enantiomers. Stereoselective interact...

Triadimefon is a systemic agricultural fungicide of the triazole class whose major metabolite, triadimenol, also a commercial fungicide, provides the majority of the actual fungicidal activity, i.e., inhibition of steroid demethylation. Both chemicals are chiral: triadimefon has one chiral center with two enantiomers while its enzymatic reduction to triadimenol produces a second chiral center a...

Stereochemistry is one of the essential dimensions in pharmacology as it dictates how enantiomers interact with biological systems. Chirality is very important in drug design. Enantiomers of the same chiral drug can have different pharmacodynamic and/or pharmacokinetic properties. In this context, replacing some existing racemates with single isomers has resulted in improved safety and/or effic...

A high-performance liquid chromatography coupled with mass spectrometry (HPLC-MS) method was established for the separation and determination of acetyl-glutamine enantiomers (acetyl-L-glutamine and acetyl-D-glutamine) simultaneously. Baseline separation was achieved on Chiralpak AD-H column (250 mm × 4.6 mm, 5 µm). n-Hexane (containing 0.1% acetic acid) and ethanol (75:25, v/v) were used as mob...

Glucocorticoids are potent anti-inflammatory and immunosuppressant agents. However, they also produce serious side effects that limit their usage. It has been proposed that anti-inflammatory properties of glucocorticoids are caused mostly by repression of activator protein 1- and nuclear factor kappabeta-stimulated synthesis of inflammatory mediators, whereas most of their adverse effects are a...

       Mefloquine (MFQ), as a racemic mixture is used for the prophylaxis and treatment of malaria. Stereoselective pharmacodynamic and pharmacokinetic differences have been observed for MFQ. In the present study, the human blood was spiked with racemic MFQ. The concentration of MFQ enantiomers in various blood fractions including packed erythrocyte layer, platelet rich plasma and platelet poor...