نتایج جستجو برای: zafirlukast
تعداد نتایج: 158 فیلتر نتایج به سال:
ATP is an important neuronal and astroglial signaling molecule in the brain. In the present study, brain slices were prepared from the prefrontal cortex (PFC) of Wistar rats and 2 lines of mice. P2X₇ receptor immunoreactivity was colocalized with astro- and microglial but not neuronal markers. Whole-cell patch-clamp recordings showed that, in astroglial cells, dibenzoyl-ATP (BzATP) and ATP caus...
The activation of purinergic receptors modulates central pattern generators controlling rhythmic motor behaviors, including respiration in rodents and swimming in frog tadpoles. The present study aimed to determine whether purinergic signaling also modulates the mammalian locomotor central pattern generator. This was investigated by using isolated spinal cord preparations obtained from neonatal...
INTRODUCTION Every year the FDA approves approximately 25 new chemical entities (NCE) which are subsequently marketed and introduced into medical and pharmaceutical practice. Many of these new compounds, such as ceftibuten (a new cephalosporin), glimepride (a new sulfonylurea), and moexepril (a new angiotensin converting enzyme inhibitor), are structurally and pharmacologically similar to curre...
The use of herbal medicines has been documented throughout recorded history including Assyrian clay tablets (2000 BC) and the Egyptian Ebers Papyrus (1550 BC) and in Ayurveda works from 900 BC. Arab scholars in Europe kept detailed notes regarding the use of medicinal plants. In the modern era, the research of natural bioactive molecules began with the isolation of morphine from opium latex in ...
Cysteinyl leukotrienes act as potent bronchoconstrictors and are part of the inflammatory cascade initiated during an asthma attack. They are produced – along with other inflammatory agents – by inflammatory cells, including mast cells and eosinophils. Leukotriene modifiers act by either inhibiting leukotriene formation (zileuton) or as leukotriene receptor antagonists (LTRAs; montelukast and z...
Genetic variants associated with asthma pathogenesis and altered response to drug therapy are discussed. Many studies implicate polymorphisms in genes encoding the enzymes responsible for leukotriene synthesis and intracellular signaling through activation of seven transmembrane domain receptors, such as the cysteinyl leukotriene 1 (CYSLTR1) and 2 (CYSLTR2) receptors. The leukotrienes are polyu...
The cysteinyl leukotrienes (CysLTs) have been implicated in the pathophysiology of inflammatory disorders, in particular asthma, for which the CysLT receptor antagonists pranlukast, zafirlukast, and montelukast, have been introduced recently as novel therapeutics. Here we report on the molecular cloning, expression, localization, and pharmacological characterization of a CysLT receptor (CysLTR)...
The drug treatment for allergic rhinitis comprises the use of intranasal corticosteroids, as well as histamine and cysteinyl leukotriene antagonists. Current guidelines advocate the use of histamine receptor antagonists for the treatment of intermittent or persistent allergic rhinitis, particularly due to seasonal pollen exposure, as these drugs have a fast onset of action (1). These drugs tend...
PURPOSE Glyoxalase I (GLO1) is an enzyme that plays a role in the detoxification of methylglyoxal, a side-product of glycolysis. We previously reported that GLO1 was a resistant factor to antitumor agent-induced apoptosis, and that S-p-bromobenzylglutathione cyclopentyl diester (BBGC), an effective inhibitor of GLO1, selectively sensitized to etoposide the drug-resistant human leukemia cells th...
Landmark clinical trials established the benefit of the thienopyridine clopidogrel, an irreversibly binding inhibitor of the platelet P2Y12 receptor, in the setting of acute coronary syndromes (ACS).1–3 Clopidogrel has thus become a key component of the current standard of care for antiplatelet therapy in the setting of ACS.4,5 Evidence has emerged, however, regarding the inherent limitations o...
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