Anesthetic Profile of a Non-lipid Propofol Nanoemulsion

SummaryBackground and objectivesThe clinical use of a lipid propofol formulation causes pain during injection, allergic reactions, and bacterial growth. Propofol has been reformulated in different non-lipid presentations to reduce the incidence of adverse effects, but those changes can modify its pharmacokinetics and pharmacodynamics. In the present study, we investigate the pharmacology and toxicology of lipid propofol (CLP) and the non-lipid nanoemulsion (NLP).MethodsConventional lipid formulation of propofol and NLP were infused in the jugular veins of rats and blood pressure (BP), heart rate (HR), and respiratory rate (RR) were measured. Both formulations (1%) were infused (40 μL.min-1) over 1 hour. Hypnotic and anesthetic doses as well as recoveries were determined. The pain induced by the CLP and NLP vehicles was compared by counting the number of abdominal contortions (“writhing test”) after the intraperitoneal (i.p.) injection in mice. Acetic acid (0.6%) was used as positive control.ResultsHypnotic and anesthetic doses of 1% CLP (6.0 ± 1.3 and 17.8 ± 2.6 mg.kg-1, respectively) and 1% NLP (5.4 ± 1.0 and 16.0 ± 1.4 mg.kg-1, respectively) were not significantly different. Recovery from hypnosis and anesthesia was faster with NLP than with CLP. Changes in HR, BP, and RR caused by NLP were not significantly different from those caused by CLP. Acetic acid and the vehicle of CLP caused 46.0 ± 2.0 and 12.5 ± 0.6 abdominal contortions 20 min after i.p. injection, respectively. The absence of abdominal contractions was observed with the vehicle of NLP. Abdominal inflammatory response was not observed after the i.p. injection of both propofol vehicles.ConclusionsNon-lipid formulation of propofol can be a better alternative to CPL for intravenous anesthesia with fewer adverse effects

Composto sulfonilidrazônico, processo de obtenção do composto sulfonilidrazônico e composições farmacêuticas

DepositadaDescreve um composto de certa fórmula, seu processo de obtenção e uso na fabricação de uma composição farmacêutica para estimular a produção de insulina. Especificamente, a presente invenção compreende uma série de sulfonilidrazonas que podem ser utilizadas na fabricação de uma composição farmacêutica para tratar diabetes. A presente invenção se situa nos campos da farmácia e da química

During muscle atrophy, thick, but not thin, filament components are degraded by MuRF1-dependent ubiquitylation

Loss of myofibrillar proteins is a hallmark of atrophying muscle. Expression of muscle RING-finger 1 (MuRF1), a ubiquitin ligase, is markedly induced during atrophy, and MuRF1 deletion attenuates muscle wasting. We generated mice expressing a Ring-deletion mutant MuRF1, which binds but cannot ubiquitylate substrates. Mass spectrometry of the bound proteins in denervated muscle identified many myofibrillar components. Upon denervation or fasting, atrophying muscles show a loss of myosin-binding protein C (MyBP-C) and myosin light chains 1 and 2 (MyLC1 and MyLC2) from the myofibril, before any measurable decrease in myosin heavy chain (MyHC). Their selective loss requires MuRF1. MyHC is protected from ubiquitylation in myofibrils by associated proteins, but eventually undergoes MuRF1-dependent degradation. In contrast, MuRF1 ubiquitylates MyBP-C, MyLC1, and MyLC2, even in myofibrils. Because these proteins stabilize the thick filament, their selective ubiquitylation may facilitate thick filament disassembly. However, the thin filament components decreased by a mechanism not requiring MuRF1

Ekrem İmamoğlu : portrait du candidat CHP à la mairie métropolitaine d’İstanbul

Tract de campagne du candidat Ekrem İmamoğlu aux élections municipales 2019 [cite] Ekrem İmamoğlu est né en 1970 dans la ville de Trabzon, sur la côte orientale de la mer Noire. Diplômé en 1992 de l’université d’Istanbul, il travaille initialement dans l’entreprise familiale, avant d’entrer en politique aux côtés du CHP, le parti kémaliste et social-démocrate. C’est sous l’étiquette du CHP qu’il est élu maire du district de Beylikdüzü à Istanbul en 2014 ((« Ekrem İmamoğlu Biyografisi », H..