Esomeprazole is commonly prescribed proton pump inhibitor for gastritis and peptic ulcer disease. Most of the time in clinical practice, phenytoin and esomeprazole are prescribed for patients of generalized seizures with concomitant peptic ulcer. Hence there are chances of drug-drug interaction because of modulations of isoenzymes CYP2C9 and CYP2C19, are involved in metabolism of phenytoin and ...

The present study aimed to assess gadoxetate disodium contrast-enhanced (CE) positron emission tomography (PET)/magnetic resonance imaging (MRI) with 68Ga-DOTATOC and 11C-5-Hydroxy-tryptophan (11C-5-HTP) in comparison iodine CE 68Ga-DOTATOC-PET/computed (CT) for neuroendocrine tumour imaging. Detection rate reader's confidence were evaluated each separate image volume: CE-CT, CE-MRI including d...

Objective: To evaluate antioxidant effect of Virgin Coconut Oil (VCO) and Corn (CO) on germinal thickness (GT) in rats induced with phenytoin toxicity. Study design setting: An Experimental Longitudinal study was done at AL-Tibri Medical College Hospital Isra University Karachi Campus. Methodology: 28 male albino were selected divided into 4 groups each consisting 7 rats. Group A received norma...

Phenytoin, 5,5-diphenylhydantoin, is a widely used anticonvulsant agent with a variety of toxicities, including drug interactions. The formation of four oxidative metabolites, 4'-hydroxylated (4'-HPPH), 3'-hydroxylated (3'-HPPH), a catechol (3',4'-diHPPH), and the 3',4'-dihydrodiol form of phenytoin was examined in rat liver microsomes. In 11 cDNA-expressed rat P450 enzymes tested, CYP2C6 had t...

Sodium-dependent glucose cotransporter 2 (SGLT2) is a pharmacological target of type 2 diabetes mellitus. The aim of this study was to noninvasively visualize the pharmacological action of a selective SGLT2 inhibitor ipragliflozin in the kidney using positron emission tomography (PET) imaging with 11C-methyl-d-glucoside (11C-MDG), an SGLT-specific radio-labeled substrate. PET imaging with 11C-M...

The 11C-monomethylstannate prepared from [11C]-methyl iodide and Lappert's stannylene, was subject to a palladium-mediated cross-coupling reaction with an aryl halide under ligand-free conditions, to afford easily purified 11C-methyl(hetero)arenes in high radiochemical yields.

Drug resistance is a major cause of chemotherapy failure in cancer treatment. One reason is the overexpression of the drug efflux pump P-glycoprotein (P-gp), involved in multidrug resistance (MDR). In vivo pharmacokinetic analysis of P-gp transport might identify the capacity of modulation by P-gp substrate modulators, such as cyclosporin A. Therefore, P-gp function was measured in vivo with po...

11C-LY2795050 is a novel k-selective antagonist PET tracer. The in vitro binding affinities (Ki) of LY2795050 at the k-opioid (KOR) and m-opioid (MOR) receptors are 0.72 and 25.8 nM, respectively. Thus, the in vitro KOR/MOR binding selectivity is about 36:1. Our goal in this study was to determine the in vivo selectivity of this new KOR antagonist tracer in the monkey. Methods: To estimate the ...

UNLABELLED Brain kappa-opioid receptors (ORs) may be involved in several pathologic conditions, such as addiction, psychosis, and seizures. (+/-)-4-Methoxycarbonyl-2-[(1-pyrrolidinylmethyl]-1-[(3,4-dichlorophenyl)acetyl]-piperidine (GR89696) is a potent and selective kappa-OR agonist. The (-)-isomer, GR103545, is the active enantiomer of GR89696. The aim of this study was to characterize the po...

The standard method of [11C]raclopride synthesis requires a large amount of its desmethyl precursor. We prepared [11C]raclopride by methylation of a small amount of desmethyl derivative (0.3-0.5 mg) with [11C]methyl iodide in a DMF solution containing NaH, with a decay-corrected radiochemical yield of 11-14% based on [11C]methyl iodide and with a specific activity of 48 TBq/mmol for 25 min from...