Search results for "antagonist"
showing 10 items of 1660 documents
Early developmental alterations of low-Mg2+ -induced epileptiform activity in the intact corticohippocampal formation of the newborn mouse in vitro.
2005
Abstract The generation, propagation and pharmacological properties of low-Mg 2+ -induced epileptiform activity were examined in the intact corticohippocampal formation (CHF) of the newborn (P0–4) mouse in vitro. Multi-site field potential recordings in dentate gyrus (DG), CA3, CA1, entorhinal cortex (EC) and temporal cortex (TC) revealed in 0.2 mM Mg 2+ -containing ACSF a stable pattern of spontaneous epileptiform activity consisting of recurrent ictal-like events (ILEs) and interictal events (IEs). Although this activity could be consistently observed as early as P0, ILEs were smaller in amplitude, less frequent and showed a slower onset in P0–2 as compared to P3–4 animals. In all age gro…
Effects of indomethacin on muscarinic inhibition of endogenous noradrenaline release from rat isolated trachea
1993
The release of endogenous noradrenaline from rat isolated tracheae was evoked by electrical field stimulation (3 Hz, 540 pulses) in the presence of yohimbine, desipramine and tyrosine. The muscarine receptor agonist oxotremorine concentration-dependently inhibited the evoked release of noradrenaline by 95% at 1 μmol/l, EC50 values in two series of experiments 41 and 57 nmol/l, respectively. The effect of oxotremorine was antagonized by the non-selective muscarine receptor antagonist scopolamine (10–1000 nmol/l) in a manner suggesting a simple competitive interaction (slope of Schild plot −0.94; pA2 value 8.88). However, the M2 selective muscarine receptor antagonist methoctramine (0.1–10 μm…
Protein kinase C-inhibiting properties of the losartan metabolite EXP3179 make the difference.
2009
The inhibition of the renin-angiotensin axis with the angiotensin II (ATII) receptor blockers, such as losartan, candesartan, and valsartan, has been demonstrated, similar to angiotensin-converting enzyme inhibitors, to reduce mortality in patients with arterial hypertension, chronic congestive heart failure, and acute myocardial infarction.1 Initially, the ATII receptor antagonist losartan helped to demonstrate new classes of ATII receptors and substantially expanded our knowledge about the cardiovascular effects of the renin-angiotensin-aldosterone system and its effector peptide ATII. Researchers dealing with this compound soon revealed that, beyond its antihypertensive effects attribute…
From structural biochemistry to expression profiling: Neuroprotective activities of estrogen
2005
Abstract Estrogens are neuromodulatory and neuroprotective hormones. Chemically, estrogens are steroid compounds and unfold most of their activities through the activation of nuclear receptors that bind to specific target genes and control their transcription. Two subtypes of estrogen receptors are known (estrogen receptor α and estrogen receptor β) and they are expressed throughout the body including the CNS and in particular the brain. We employed large scale DNA-chip-analysis to display the gene expression pattern differentially regulated by both estrogen receptor subtypes in human neuronal cells. We identified different gene families regulated by estrogen receptors that complement the k…
Inducibility of the avidin gene by progesterone is suppressed during estrogen-induced cytodifferentiation.
1992
Abstract We have studied epithelial differentiation of the chick oviduct as induced by diethylstilbestrol (DES) and 17β-estradiol (E 2 ). The proportion of goblet cells in the oviduct was slightly higher after E 2 than after DES treatment. Also avidin induction by progesterone was stronger following DES than E 2 priming. In the estrogen pretreated oviduct epithelium, avidin expression was induced by progesterone in the surface epithelial cells, protodifferentiated gland cells and tubular gland cells, but not in goblet cells. During prolonged estrogen treatment, however, the inducibility of avidin by progesterone ceased in tubular gland cells but not in surface epithelial cells. The estrogen…
Genetic variants of ANP and cardiometabolic protection: from populations to novel therapeutics
2013
Background The cardiac hormone atrial natriuretic peptide (ANP) induces natriuresis, vasodilation and inhibits aldosterone through the activation of the guanylyl cyclase A receptor (GC-A) and the second messenger cGMP. ANP possesses also metabolic properties enhancing lipolysis and release of the adipokine adiponectin. Previous studies in general populations reported that the minor G allele of the ANP genetic variant rs5068 is associated with increased circulating levels of ANP and B-type natriuretic peptide, lower blood pressure (BP), and reduced risk of hypertension. We recently reported that in the general population from Olmsted County, MN, USA the G allele of rs5068 is associated not o…
Medical treatment for inoperable malignant bowel obstruction: a qualitative systematic review.
2007
The use of symptomatic agents has greatly improved the medical treatment of advanced cancer patients with inoperable bowel obstruction. A systematic review of studies of the most popular drugs used in the medical management of inoperable malignant bowel obstruction was performed to assess the effectiveness of these treatments and provide some lines of evidence. Randomized trials that involved patients with a clinical diagnosis of intestinal obstruction due to advanced cancer treated with these drugs were reviewed. Five reports fulfilled inclusion criteria. Three studies compared octreotide (OC) and hyoscine butylbromide (HB), and two studies compared corticosteroids (CSs) and placebo. Globa…
Airway Deposition of Extrafine Inhaled Triple Therapy in Patients with COPD: A Model Approach Based on Functional Respiratory Imaging Computer Simula…
2020
Omar S Usmani,1 Nicola Scichilone,2 Benjamin Mignot,3 Dennis Belmans,3 Cedric Van Holsbeke,3 Jan De Backer,3 Roberta De Maria,4 Erika Cuoghi,4 Eva Topole,4 George Georges4 1Airway Disease Section, National Heart and Lung Institute, Imperial College, London, UK; 2PROMISE Department of Medicine, University of Palermo, Palermo, Italy; 3FLUIDDA, Kontich, Belgium; 4Chiesi Farmaceutici, SpA, Parma, ItalyCorrespondence: George GeorgesChiesi USA Inc., 175 Regency Woods Place, Ste. 600, Cary, NC 27518, USATel +1 (919) 678 6611 x1536Email george.georges@chiesi.comIntroduction: There is a clear correlation between small airways dysfunction and poor clinical outcomes in patients with chronic obstructiv…
Activation of mGlu3 Receptors Stimulates the Production of GDNF in Striatal Neurons
2009
Metabotropic glutamate (mGlu) receptors have been considered potential targets for the therapy of experimental parkinsonism. One hypothetical advantage associated with the use of mGlu receptor ligands is the lack of the adverse effects typically induced by ionotropic glutamate receptor antagonists, such as sedation, ataxia, and severe learning impairment. Low doses of the mGlu2/3 metabotropic glutamate receptor agonist, LY379268 (0.25-3 mg/kg, i.p.) increased glial cell line-derived neurotrophic factor (GDNF) mRNA and protein levels in the mouse brain, as assessed by in situ hybridization, real-time PCR, immunoblotting, and immunohistochemistry. This increase was prominent in the striatum, …
Antagonizing dabigatran by idarucizumab in cases of ischemic stroke or intracranial hemorrhage in Germany—Updated series of 120 cases
2020
Background Idarucizumab is a monoclonal antibody fragment with high affinity for dabigatran reversing its anticoagulant effects within minutes. Thereby, patients with acute ischemic stroke who are on dabigatran treatment may become eligible for thrombolysis with recombinant tissue-type plasminogen activator (rt-PA). In patients on dabigatran with intracerebral hemorrhage idarucizumab could prevent lesion growth. Aims To provide insights into the clinical use of idarucizumab in patients under effective dabigatran anticoagulation presenting with signs of acute ischemic stroke or intracranial hemorrhage. Methods Retrospective data collected from German neurological/neurosurgical departments ad…