Tenofovir (TFV), a first-line anti-viral agent, has been prepared as various forms of prodrugs for better bioavailability, lower systemic exposure and higher target cells loading of TFV to enhance efficacy and reduce toxicity. TFV undergoes intracellular phosphorylation to form TFV diphosphate (...

A liquid chromatography with triple quadrupole mass spectrometry method was developed and validated for the determination of tenofovir and tenofovir alafenamide concentrations in human plasma and cerebrospinal fluid. Tenofovir and tenofovir alafenamide were extracted from matrix by solid phase e...

Tenofovir-associated renal toxicity is influenced by several factors, including plasma exposure and genetic variants in transporter-encoding genes. Tenofovir plasma exposure has been associated with a polymorphism in SLC28A2 gene (encoding the concentrative nucleoside transporter 2, CNT2): parti...

An ultra performance liquid chromatography-tandem mass spectrometric (UHPLC-MS/MS) method has been developed for the simultaneous determination of tenofovir alafenamide (TAF) and it's metabolite tenofovir (TFV) in human plasma. The analytes and inter standards, TAF-d5 and TFV-d6 were extrac...

Angiotensin-(1–7) [Ang-(1–7)] exhibits blood pressure lowering actions, inhibits cell growth, and reduces tissue inflammation and fibrosis which may functionally antagonize an activated Ang II-AT1 receptor axis. Since the vascular actions of Ang-(1–7) and the associated receptor/signaling pat...

Conformational analysis of α(I) and β(II) epimers of 3-phenethyl-3-azabicyclo [3.2.1] octan-8-ol has been performed using the Molecular Mechanics Method (MM2). In both cases, the global minimum-energy conformer was the slight distorted chair form with the N-phenethyl group in equatorial positi...

Physostigmine (PHY) has the advantage over pyridostigmine of minimizing OP-induced incapacitation because it penetrates into the CNS. However, physostigmine is behaviorally toxic at relatively low concentrations. It is anticipated that this could be offset by a cholinolytic to prevent behavioral...

The effects of the muscarinic acetylcholine receptor antagonists, azaprophen (0.3–10.0 mg/kg), scopolamine (0.01–3.0 mg/kg) and trihexyphenidyl (0.3–10.0 mg/kg) were examined in rats using a VI 18 s schedule of food reinforcement, before and after chronic physostigmine administrarion. All thr...

The effects of the anticholinergic atropine and azaprophen, a novel, conformationally restricted analog of atropine, were examined in rhesus monkeys using delayed match-to-sample and detection tasks. Both compounds (0.01–0.32 mg/kg) produced dose-dependent decreases in the rate of responding un...

To date, 5-hydroxytryptamine1A (5-HT1A) receptor-mediated functional assays (adenylyl cyclase inhibition, high-affinity GTPase activity and [35S]guanosine-5′-O-(γ-thio)-triphosphate ([35S]GTPγS) binding) have been performed mainly in hippocampal membranes. In the current study, 5-HT-stimulate...

G protein-coupled receptors exist in G protein-coupled and -uncoupled forms that exhibit high and low affinity for agonists, respectively. Consequently, affinity differences of a compound for the high vs. the low affinity state of a receptor have been used to estimate its intrinsic activity at t...

A sustained-release parenteral formulation of granisetron hydrochloride, a water-soluble drug, was developed in the form of an oil suspension loaded with microparticles. Spray drying technique was employed to prepare microparticles of polymers and the drug without using organic solvents. The eff...

A highly sensitive and selective high-performance liquid chromatographic method was developed for the determination of granisetron and its active metabolite, 7-hydroxygranisetron (7OH-G) in human plasma. Granisetron is a selective 5-hydroxtryptamine receptor antagonist used in the treatment of c...

In this paper separation of granisetron and its two related substances in HILIC mode is presented. Separation was done on silica column derivatized with sulfoalkylbetaine groups (ZIC-HILIC). Firstly, retention mechanisms were assessed whereby retention factors of substances were followed in wide...

The aim of this study was to investigate the effects of adding maleic anhydride grafted polypropylene (MA-PP) and graphite nanoplatelets (GNPs) into polypropylene. The tensile strength and flexural properties of the GNP/PP composite were enhanced with an increase in the MA-PP content and the GNP...

The fracture properties of melt-mixed polyamide-6 (PA-6)/polypropylene grafted maleic anhydride (PP-g-MA)/nanoclay ternary nanocomposites were investigated following essential work of fracture (EWF) approach based on post-yield fracture mechanics principles. Fourier transform infrared (FTIR) spe...

The influence of epoxy resin (EP) and maleic anhydride grafted polypropylene (PPMA) on mechanical properties of polypropylene/short carbon fiber (PP/SCF) composites was studied. The combination between EP and PPMA showed a synergistic effect on improving the mechanical properties of PP/SCF compo...

The morphology of polypropylene (PP)/polyamide 66 (PA66) blend at an asymmetric composition is tailored by organoclay and maleic anhydride grafted polypropylene (MAPP). Without MAPP, a transition from typical sea-island morphology to coarse co-continuous morphology is observed when organoclay lo...

The morphology and thermal behaviour of polypropylene–graft–maleic anhydride (PP–g–MA) layered silicate (montmorillonite) nanocomposites were investigated using X-ray diffraction, transmission electron microscopy, differential scanning calorimetry and thermogravimetry. The study focuses on t...

The octadecylamine (ODA) modified graphene oxide (mGO-ODA)/maleic anhydride grafted polypropylene (MAPP) composites (mGO-ODA/MAPP) were prepared and applied successfully as gas barrier and corrosion protection coating materials for the first time. The hydrophobic mGO-ODA sheets showed improved s...