Abstract:
:Pyrimidine nucleotides, including UTP, UDP and UDP-glucose, are important signaling molecules which activate G protein-coupled membrane receptors of the P2Y family. Four distinct pyrimidine nucleotide-sensitive P2Y receptor subtypes have been cloned, P2Y(2), P2Y(4), P2Y(6) and P2Y(14). Pharmacological experiments indicate that further subtypes may exist. P2Y(2) and P2Y(4) receptors are activated by UTP (the P2Y(2) and the rat, but not the human P2Y(4) receptor are also activated by ATP), the P2Y(6) receptor is activated by UDP, and the P2Y(14) receptor by UDP-glucose. Derivatives and analogs of the physiological nucleotides UTP, UDP and ATP have been synthesized and evaluated in order to obtain enzymatically stable, subtype-selective agonists. P2Y(2) agonists are currently in clinical development for cystic fibrosis and dry eye syndrome. Selective antagonists for pyrimidinergic P2Y receptors are still lacking.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Müller CEdoi
10.2174/1381612023392937subject
Has Abstractpub_date
2002-01-01 00:00:00pages
2353-69issue
26eissn
1381-6128issn
1873-4286journal_volume
8pub_type
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journal_title:Current pharmaceutical design
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doi:10.2174/1381612822666151112152143
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journal_title:Current pharmaceutical design
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abstract::Stroke is a leading cause of death and disability worldwide. Conventional treatment has a limitation of very narrow therapeutic time window and its devastating nature necessitate a novel regenerative approach. Transplanted stem cells resulted in functional recovery through multiple mechanisms including neuroprotection...
journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
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abstract::The endocannabinoid system (ECS) is now recognised as an important modulator of various central nervous system processes. More recently, an increasing body of evidence has accumulated to suggest antioxidant, anti-inflammatory and neuroprotective roles of ECS. In this review we discuss the role and therapeutic potentia...
journal_title:Current pharmaceutical design
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abstract:PURPOSE:Ultrasound contrast agents involving a therapeutic drug applied during enhanced imaging can be used for targeted therapy. The preparation of contrast agents is a precondition and basis for the use of multifunctional contrast agents in molecular imaging. METHODS:This study uses thin-film hydration-mechanical vi...
journal_title:Current pharmaceutical design
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abstract::Gene delivery, a process of introducing foreign functional nucleic acids into target cells, has proven to be a very promising tool for inducing specific gene expression in host cells. Many different technologies have been developed for efficient gene delivery. Among them, electroporation has been adopted in gene deliv...
journal_title:Current pharmaceutical design
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abstract::Mediation of antinociception via opioid receptors located in the periphery is a viable strategy to produce analgesia without the occurrence of side effects associated with stimulation of opioid receptors located in the central nervous system. Peripheral opioid receptors are particularly important in inflammatory pain ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::The activities of individual cells must be tightly coordinated in order to build and maintain complex 3- dimensional body structures during embryogenesis and regeneration. Thus, one way to view cancer is within systems biology as a network disorder affecting the ability of cells to properly interact with a morphodynam...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract:BACKGROUND:Non-alcoholic fatty liver disease (NAFLD) is one of the most common causes of chronic liver disease worldwide directly related to the progressive increase in overweight and obesity. The accumulation of lipids in patients with NAFLD contributes to the development of insulin resistance, inflammatory response a...
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abstract::Sulphur mustard (SM; (2, 2'-dichloroethylsulfide)) was used for the first time in 1917, during the World War I. SM mainly induces DNA damage, oxidative stress, and inflammation. This compound injures the respiratory system, eyes, skin and the endocrine, gastrointestinal, and hematopoietic systems. However, due to the ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::Macrophages are professional scavengers of apoptotic and necrotic cells, and hence constantly take up self antigens. Paradoxically, macrophages are also professional antigen-presenting cells, which would seem to invite autoimmune disorders. Moreover, macrophages are effector cells in the tissue-destruction phase of au...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2003-01-01 00:00:00
abstract::Myocarditis is a disease whose pathogenesis is not completely understood and whose prevalence is likely underestimated. Individuals afflicted with this condition may be treated with agents that relieve symptoms arising from inflammation and concurrent cellular damage. One class of drugs commonly used in the treatment ...
journal_title:Current pharmaceutical design
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abstract::The use of systematic approach for the analysis of mechanism of action of drugs at different levels of biological organization of organisms is an important task in experimental and clinical pharmacology for drug designing and increasing the efficacy and safety of drugs. The analysis of published data on pharmacologica...
journal_title:Current pharmaceutical design
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abstract::Pulmonary surfactant, a complex of lipids and proteins, functions to keep alveoli from collapsing at expiration. Surfactant proteins A (SP-A) and D (SP-D) belong to the collectin family and play pivotal roles in the innate immunity of the lung. Pulmonary collectins directly bind with broad specificities to a variety o...
journal_title:Current pharmaceutical design
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更新日期:2006-01-01 00:00:00
abstract::DNA methylation, a major regulator of epigenetic modifications has been shown to alter the expression of genes that are involved in aspects of glucose metabolism such as glucose intolerance, insulin resistance, β-cell dysfunction and other conditions, and it ultimately leads to the pathogenesis of type 2 diabetes mell...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::Providing novel treatments to help cancer patients live longer and have better lives remains one of the biggest challenges of the pharmaceutical industry. Today much is known about the molecular and genetic causes of cancers thus facilitating the development of novel targeted cancer drugs with improved risk-benefit ra...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::The intracellular hydric balance is an essential process of mammalian cells. The water movement across cell membranes is driven by osmotic and hydrostatic forces and the speed of this process is dependent on the presence of specific aquaporin water channels. Since the molecular identification of the first water channe...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::The metabolic syndrome (MetS) represents a cluster of medical disorders, such as hyperglycemia, dyslipidemia, hypertension, and abdominal obesity that, when occurring together, increase the risk of developing cardiovascular disease. The role of food and nutrients in the aetiology of chronic diseases has become clearer...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract:BACKGROUND:R. Schofield (1978) proposed a hypothesis of hematopoietic stem cells (HSCs) niche (specialized cell microenvironment). An existence of osteoblastic and vascular niches for HSCs has been postulated since 2003. At the same time, the discussion about the existence and functioning of niche for multipotent mesen...
journal_title:Current pharmaceutical design
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更新日期:2018-01-01 00:00:00
abstract::Chronic pain is a widespread healthcare problem affecting not only the patient but in many ways all the society. Chronic pain is a disease itself that endures for a long period of time and it is resistant to the majority of medical treatments that provide modest improvements in pain and minimum improvements in physica...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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abstract::Metabolic syndrome (MetS) which is caused by poor dietary habits and sedentary behavior is a serious global health problem. MetS is a cluster of risk factors, represented by central obesity, hyperglycemia, dyslipidemia, and hypertension. In the 21st century, MetS and associated comorbidities, including obesity, diabet...
journal_title:Current pharmaceutical design
pub_type: 社论
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abstract::The majority of pharmaceutical formulations for the treatment of ocular pathologies are for topical administration. However, this kind of ophthalmic formulations has disadvantages such as low bioavailability and, consequently, a reduced therapeutic effect. This happens due to the anatomical and physiological specifici...
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更新日期:2015-01-01 00:00:00
abstract:BACKGROUND:Human brain is amongst the most complex organs in human body, and delivery of therapeutic agents across the brain is a tedious task. Existence of blood brain barrier (BBB) protects the brain from invasion of undesirable substances; therefore it hinders the transport of various drugs used for the treatment of...
journal_title:Current pharmaceutical design
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abstract::Mast cells, traditionally regarded as effector cells of the immune system, have more recently been demonstrated to be key figures in initiating, developing and sustaining complex pathophysiological processes underlying asthma and other allergic diseases. Asthma is characterised by airway inflammation alongside a distu...
journal_title:Current pharmaceutical design
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更新日期:2011-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVE:Bevacizumab (BVZ) is a recombinant humanized antibody that inhibits the vascular endothelial growth factor A (VEGFA) and is used for the treatment of various types of cancer. BVZ is primarily given by the intravenous drip (I.V.), which often leads to low efficacy and various side effects. There...
journal_title:Current pharmaceutical design
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更新日期:2019-01-01 00:00:00
abstract::The survival of patients with pulmonary arterial hypertension is closely related with right ventricular function. During the progression of right ventricular remodeling, energetic metabolism shifts from oxidative mitochondrial metabolism to glycolysis. In normal physiological conditions, cardiomyocytes use major sourc...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2016-01-01 00:00:00