A new strategy for converting antipsychotic drug olanzapine into PDE4 inhibitors is described via the design and Pd/C mediated synthesis of novel N-indolylmethyl olanzapine derivatives. One compound ...showed good inhibition (IC50 1.1 μM) and >10 fold selectivity towards PDE4B over D that was supported by docking studies. This compound also showed significant inhibition of TNF-α and no major toxicities in cell lines and a zebrafish embryo model except the teratogenic effects to be re-assessed in rodents.
A selective, sensitive, high pressure liquid chromatography-positive electrospray ionization tandem mass spectrometry method was developed and validated for the quantification of aripiprazole in ...human K2EDTA plasma using zolpidem tartrate as an internal standard. The analyte and internal standard were extracted from human plasma by solid-phase extraction using methanol. The eluted samples were chromatographed on a Grace Smart RP 18 4.6 × 100 mm, 3 µ column by using a 95:5 v/v mixture of methanol and ammonium acetate buffer (30 mM, pH 5.0 ± 0.05) as a gradient mobile phase at a flow rate of 0.6 mL/min, and analyzed by mass spectrometry in the multiple reaction monitoring mode using the M + H+ ions m/z 448.03 → 285.14 for aripiprazole and m/z 308.13 → 235.25 for the internal standard (zolpidem tartrate), respectively. Calibration plots were linear over the concentration range of 0.20 to 60.01 ng/mL. Intra-day and inter-day precision (percent coefficient of variation) and accuracy (percent nominal) for quality control samples (0.60, 30.60 and 45.59 ng/mL) ranged between 2.28 and 8.93% and between 92.50 and 107.07%, respectively. Extraction recovery of aripiprazole from plasma was in the range 75.56-79.57%; mean recovery was 77.35%. The main pharmacokinetic parameters were Tmax = (4.00 ± 2.336) Cmax = (55.16 ± 13.490) and AUC = (1846.28 ± 484.686).
Cucurbita pepo as a Coagulant Aid for Copper Removal P. Deepthi; P. Sharath Kumar; Dr. C. Sarala ...
International journal of engineering research & technology (Ahmedabad),
09/2017, Letnik:
6, Številka:
9
Journal Article
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