Search results for "Amide"
showing 10 items of 3119 documents
The effects of LSD in the guinea-pig ileum
1985
The effects of lysergic acid diethylamide (LSD) on acetylcholine release and on smooth muscle tone were studied in the myenteric plexus-longitudinal muscle preparation of the guinea pig. LSD (0.01-10 microM) depressed in a concentration-dependent manner the electrically-evoked [3H]-acetylcholine outflow from strips preincubated with [3H]-choline. The maximal effect was a 45% inhibition by 1 microM LSD. The spontaneous outflow was not affected. Metitepine competitively antagonized (pA2 8.0) the LSD-induced reduction of the evoked outflow. Tolazoline and mepyramine did not affect the inhibitory action of LSD. The contractions in response to electrical stimulation were enhanced by 34% in the p…
HCV cirrhosis at the edge of decompensation: Will paritaprevir with ritonavir, ombitasvir, dasabuvir, and ribavirin solve the need for treatment?
2014
BACKGROUND: The interferon-free combination of the protease inhibitor ABT-450 with ritonavir (ABT-450/r) and the NS5A inhibitor ombitasvir (also known as ABT-267) plus the nonnucleoside polymerase inhibitor dasabuvir (also known as ABT-333) and ribavirin has shown efficacy against the hepatitis C virus (HCV) in patients with HCV genotype 1 infection. In this phase 3 trial, we evaluated this regimen in previously untreated patients with HCV genotype 1 infection and no cirrhosis. METHODS: In this multicenter, randomized, double-blind, placebocontrolled trial, we assigned previously untreated patients with HCV genotype 1 infection, in a 3:1 ratio, to an active regimen consisting of a single-ta…
The Oxidative Stress Concept of Nitrate Tolerance and the Antioxidant Properties of Hydralazine
2005
The hemodynamic and anti-ischemic effects of nitroglycerin (NTG) are rapidly blunted as a result of the development of nitrate tolerance. With initiation of NTG therapy, it is possible to detect neurohormonal activation and intravascular volume expansion. These so-called pseudotolerance mechanisms may compromise the vasodilatory effects of NTG. Long-term nitrate treatment also is associated with decreased vascular responsiveness caused by changes in intrinsic mechanisms of the tolerant vasculature itself. According to the oxidative stress concept, increased vascular superoxide (O 2 − ) production and an increased sensitivity to vasoconstrictors secondary to activation of protein kinase C co…
Brinzolamide/brimonidine fixed-dose combination bid as an adjunct to a prostaglandin analog for open-angle glaucoma/ocular hypertension.
2019
Purpose: To evaluate the additive intraocular pressure–lowering effect of twice-daily brinzolamide 1%/brimonidine 0.2% fixed-dose combination (BBFC) as an adjunct to a prostaglandin analog (PGA) in patients with open-angle glaucoma or ocular hypertension insufficiently controlled with PGA monotherapy. Methods: In this Phase 4, double-masked trial, patients aged ⩾18 years, with a mean intraocular pressure of ⩾19 and <32 mm Hg in at least one eye were randomized (1:1) to receive BBFC + PGA ( n = 96) or vehicle + PGA ( n = 92) for 6 weeks. The primary endpoint was the mean change in diurnal intraocular pressure from baseline (averaged over 09:00 and 11:00 h) at Week 6. Results: The mean diu…
The involvement of MMP-2 and MMP-9 in heart exercise-related angiogenesis
2013
Background Little is known about the involvement of matrix metalloproteinases (MMPs) in cardiac vascular remodelling induced by exercise. Our aim was to evaluate and localize MMP-2 and MMP-9’s activities in relation to capillary proliferation in mouse hearts trained for 15, 30 and 45 days. Methods Sixty-three mice were randomly assigned to 7 groups: four control sedentary groups (C0, C15, C30 and C45) and three groups trained by an endurance protocol (T15, T30 and T45). MMP-2 and MMP-9 were examined with zymography and immunostaining analyses. Capillary proliferation was evaluated counting the number of CD31-positive cells. Results Different activity patterns of the latent form of both MMPs…
The Role of Tumor Volume in ‘Reoxygenation’ upon Cyclophosphamide Treatment
1995
The effect of cyclophosphamide (CP) injection (60 mg/kg i.p., single dose) on volume growth and tissue oxygenation (pO2 distribution) was investigated in rat DS-sarcomas. CP was administered 4 days after subcutaneous (s.c.) tumor implantation (volume approximately 0.35 ml). Polarographic pO2 measurements were performed in the subcutis at the hind foot dorsum and in tumors 72 h after CP administration. The oxygenation status of these tissues was compared with that of saline-treated controls. CP-injection caused a mean growth delay of 11 days in DS-sarcomas and had no impact on the oxygenation status of the subcutis. In contrast, in s.c. growing DS-sarcomas the pO2 distribution improved signi…
Fabry disease defined: baseline clinical manifestations of 366 patients in the Fabry Outcome Survey.
2004
Background Fabry disease is a rare X-linked disorder caused by deficient activity of the lysosomal enzyme α-galactosidase A. Progressive accumulation of the substrate globotriaosylceramide in cells throughout the body leads to major organ failure and premature death. In response to the recent introduction of enzyme replacement therapy, the Fabry Outcome Survey (FOS) was established to pool data from European clinics on the natural history of this little-known disease and to monitor the long-term efficacy and safety of treatment. This paper presents the first analysis of the FOS database and provides essential baseline data against which the effects of enzyme replacement can be measured. De…
Effects of nicotinamide adenine dinucleotide hydride on physical and mental performance
2007
The aim of this study was to assess the effects of nicotinamide adenine dinucleotide hydride (NADH) on maximal oxygen uptake (VO2max), maximal anaerobic running time, and mental performance. Eight men were exposed to a supplement treatment (30 mg NADH as ENACHI tablets per day) and to a placebo treatment, each of 4 weeks' duration, in a balanced, double-blind, and cross-over design. The two treatments were separated by a 14-week wash-out period. The results indicated that VO2max, maximal anaerobic running time, and the ability to concentrate were similar in the NADH and placebo conditions. There were also no differences in blood lactate, creatine kinase, reaction time or feelings of fatigue…
Vitellogenin polypeptide levels in one susceptible and one cadmium-resistant strain of Oncopeltus fasciatus (Heteroptera: Lygaeidae), and its role in…
2005
The heavy metal Cd has recently been shown to have endocrine disrupting activity in different vertebrate species. In the insect Oncopeltus fasciatus, Cd exposure delays ovarian maturation and inhibits vitellogenesis, probably through a reduction in vitellogenin (Vg) polypeptide synthesis. An O. fasciatus strain was selected in the laboratory for Cd resistance with gradually increasing Cd concentrations for 50 generations. Cd-selected (OCdR) insects were 2.7-2.3 times more resistant to chronic exposure to Cd than susceptible (OS) insects. OCdR females showed increased (up to 90%) Vg polypeptide levels in hemolymph. Vg polypeptide synthesis was equally decreased in OCdR and OS females after a…
Acute ammonia intoxication induces an NMDA receptor-mediated increase in poly(ADP-ribose) polymerase level and NAD+ metabolism in nuclei of rat brain…
2004
Acute ammonia toxicity is mediated by excessive activation of NMDA receptors. Activation of NMDA receptors leads to activation of poly(ADP-ribose) polymerase (PARP) which mediates NMDA excitotoxicity. PARP is activated following DNA damage and may lead to cell death via NAD+ and ATP depletion. The aim of the present work was to assess whether acute ammonia intoxication in vivo leads to increased PARP in brain cells nuclei and to altered NAD+ and superoxide metabolism and the contribution of NMDA receptors to these alterations. Acute ammonia intoxication increases PARP content twofold in brain cells nuclei.NAD+ content decreased by 55% in rats injected with ammonia. This was not due to decre…