Search results for "Azepine"

Standard additions-dilution method for absolute quantification in voltammetry of microparticles. Application for determining psychoactive 1,4-benzodi…

2013

A standard additions-dilution solid-state electrochemical method for the determination of psychoactive 1,4-benzodiazepine and antidepressants drugs used as adulterants in commercial slimming herbal formulations is described and compared with conventional standard addition method. The proposed method, based on the voltammetry of microparticles approach, permits quantify, via standard additions methodology, 1,4-benzodiazepine and antidepressants drugs in phytotherapeutic formulations with no need of sample dissolution using dilution with a reference electroactive compound. The method was used to measure 1,4-benzobenzodiazepines (clonazepam, flurazepam, alprazolam, midazolam, bromazepam, chlor…

Efficacy of BET Bromodomain Inhibition in Kras-Mutant Non–Small Cell Lung Cancer

2013

Abstract Purpose: Amplification of MYC is one of the most common genetic alterations in lung cancer, contributing to a myriad of phenotypes associated with growth, invasion, and drug resistance. Murine genetics has established both the centrality of somatic alterations of Kras in lung cancer, as well as the dependency of mutant Kras tumors on MYC function. Unfortunately, drug-like small-molecule inhibitors of KRAS and MYC have yet to be realized. The recent discovery, in hematologic malignancies, that bromodomain and extra-terminal (BET) bromodomain inhibition impairs MYC expression and MYC transcriptional function established the rationale of targeting KRAS-driven non–small cell lung cance…

Phase I Assessment of New Mechanism-Based Pharmacodynamic Biomarkers for MLN8054, a Small-Molecule Inhibitor of Aurora A Kinase

2011

Abstract The mitotic kinase Aurora A is an important therapeutic target for cancer therapy. This study evaluated new mechanism-based pharmacodynamic biomarkers in cancer patients in two phase I studies of MLN8054, a small-molecule inhibitor of Aurora A kinase. Patients with advanced solid tumors received MLN8054 orally for 7 consecutive days in escalating dose cohorts, with skin and tumor biopsies obtained before and after dosing. Skin biopsies were evaluated for increased mitotic cells within the basal epithelium. Tumor biopsies were assessed for accumulation of mitotic cells within proliferative tumor regions. Several patients in the highest dose cohorts showed marked increases in the ski…

Cholinesterase Activity and Hematological Parameters as Biomarkers of Sublethal Molinate Exposure in Anguilla anguilla

2000

Cholinesterase (ChE) activity was measured in plasma, whole blood [using 5,5'-dithiobis(2-nitrobenzoic acid) and 2-PDS as chromophores], brain, and whole eyes of Anguilla anguilla exposed to a sublethal concentration of 11.15 mg/L (one-third of the 96-h LC(50)) of the carbamate herbicide molinate. ChE activity was evaluated after 6, 24, 48, 72, and 96 h of pesticide exposure. Results indicated that ChE activity in eel tissues decreased as time of exposure increased, especially in eel blood. Eels exposed to molinate were transferred to a pesticide-free water for a recovery period of 4 days and ChE activity was also evaluated. Results indicated that ChE activity for those animals with preexpo…

Effect of genetics polymorphism of carbamazepine – metabolizing enzymes in epileptic patients

2013

Transbuccal tablets of carbamazepine: formulation, release and absorption pattern.

2006

Tranbsuccal drug administration is an attractive method, as it has several advantages especially with respect to peroral delivery. Here we report: i) the aptitude of carbamazepine (CBZ) to penetrate porcine buccal mucosa and reconstituted human oral (RHO) epithelium; ii) three different tablet formulations for transbuccal administration; iii) the drug release rate from tablets. CBZ permeation through the buccal mucosa was investigated by using two different bi-compartmental open models: Franz cells for porcine buccal mucosa and Transwell diffusion cells system for RHO epithelium. Results, expressed as drug flux (Js) and permeability coefficients (Kp), indicated that CBZ well penetrates the …

Buccal Delivery of Carbamazepine (CBZ): a New Scenario in Menagement of Trigeminal Neuralgia (TN)

2008

Somministrazione transbuccale vs somministrazione endovenosa della Galantamina: studio sperimentale in vivo

2008

The lack of the effect of DA-1 and DA-2 dopamine agonists on the isolated guinea-pig atria.

1987

1 The effects of dopamine and both DA-1 and DA-2 dopamine receptor agonists have been studied on the contractile force of electrically driven guinea-pig left atria and frequency of spontaneously beating right atria. 2 Pretreatment of animals with reserpine caused a parallel rightward shift of the concentration-response curve to dopamine of either preparation. 3 Propranolol, but not domperidone, shifted to the right the dose-response curve for the positive inotropic and chronotropic effects of dopamine. 4 Neither apomorphine, fenoldopam, bromocriptine nor piribedil had effects on the frequency and contractile force of the isolated guinea-pig atria. 5 These results suggest that DA-1 and DA-2 …

Influence of pH on the benzodiazepine-human serum albumin complex. Circular dichroism studies.

1974

The influence of pH on the binding of benzodiazepine derivatives to HSA was studied by circular dichroism measurements and by gel filtration. The binding of nearly all benzodiazepines is increased by rising the pH from 6.60 to 8.20. For flurazepam, clonazepam, and nitrazepam this increase in binding is due to an increase of the affinities, while for the other substances the affinity remains constant and the number of binding sites is increased from one to two. The changes in binding of the benzodiazepines by rising the pH are explained by a cationic amino acid residue near or at the benzodiazepine binding site of the HSA molecule. This second binding site is not detectable by circular dichr…