Abstract:
:The activation of Corticotrophin Releasing-Factor (CRF) receptors in the brain is well established to coordinate the endocrine, behavioral, autonomic and visceral responses to stress. In addition, CRF receptors are also expressed within the gut where they exert biological actions and play a role in modulating stress-related gastrointestinal function. In particular, peripheral injection of CRF and related peptides, urocortin 1, 2 or 3 inhibit Gastric Emptying (GE) and alters fasted and fed pattern of gastroduodenal motility in several experimental species. Urocortin 1 interacts synergistically with cholecystokin-8 to inhibit gastric emptying in lean mice which is no longer observed in diet-induced obese rats. In in vitro circular or longitudinal muscle preparation of rat antrum, CRF and urocortin 1 and 2 suppressed spontaneous contractile activity. CRF and urocortins interact with the CRF receptor 2 (CRF-R2) to inhibit gastric motor function monitored both in vivo and in vitro. The CRF-R2 mediated inhibition of antral and corpus contractility involves a direct action on gastric myenteric neurons where CRF-R2 is expressed and may also involve the activation of serotonin acting on 5-HT3 receptor. The involvement of peripheral CRF receptors in gastric motor alterations occurring under stress conditions are stressors specific with CRF-R2 mediating the early phase of gastric ileus induced by abdominal surgery and the delayed emptying elicited by acute restraint stress. However gastric stasis elicited by endotoxin is not mediated by CRF-R2 and CRF receptors are not involved in the basal regulation of fed or fasted pattern of gastric motility.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Czimmer J,Tache Ydoi
10.2174/1381612823666170228142428subject
Has Abstractpub_date
2017-01-01 00:00:00pages
4042-4047issue
27eissn
1381-6128issn
1873-4286pii
CPD-EPUB-82048journal_volume
23pub_type
杂志文章,评审abstract::In recent years, nanosuspensions have been accepted as a valuable drug delivery system for poorly water-soluble drugs. Topdown and bottom-up technologies are the two main approaches for generating nanosuspensions. Several products manufactured by the top-down technologies have been successfully commercialized demonstr...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990401
更新日期:2014-01-01 00:00:00
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
doi:10.2174/138161282639201110165712
更新日期:2020-01-01 00:00:00
abstract::Macrophage migration inhibitory factor (MIF) is a pro-inflammatory cytokine released from T-cells and macrophages, and is a key molecule in inflammation. Although a detailed understanding of the biological functions of MIF has not yet been found, it is known that MIF catalyzes the tautomerization of phenylpyruvate and...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612023394674
更新日期:2002-01-01 00:00:00
abstract:BACKGROUND:Mitochondria are cellular organelles responsible for energy production, calcium handling, controlled synthesis of reactive oxygen species (ROS), and regulation of apoptosis. All these functions are crucial for cardiac homeostasis, and may be impaired in chronic heart failure (CHF). Therefore, mitochondrial d...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160701075027
更新日期:2016-01-01 00:00:00
abstract::Inhibition of carbonic anhydrase (CA, EC 4.2.1.1) isoforms present in the eyes (CA I, II, IV and XII), with sulfonamides such as acetazolamide, methazolamide, ethoxzolamide and dichlorophenamide, is still widely used for the systemic treatment of glaucoma. The mechanism of action of these drugs consists in inhibition ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161208783877866
更新日期:2008-01-01 00:00:00
abstract::The octapeptide angiotensin II (Ang II) plays a homeostatic role in the regulation of blood pressure and water and electrolyte balance, and also contributes to the progression of cardiovascular remodeling. Ang II activates Ang II type 1 (AT1) receptor and type 2 (AT2) receptor, both of which belong to the seven-transm...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811319170003
更新日期:2013-01-01 00:00:00
abstract::Neurodegenerative disorders are one of the most critical public health concerns of our times. Regrettably, therapeutic interventions currently available have shown only partial benefits to patients affected by one of these disorders. Although the important advances made during the last decades, several questions regar...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666151223103038
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Clinic resting heart rate (RHR), is one of the cardiovascular parameters more easily measurable. In the general population RHR has been associated with total and cardiovascular mortality and higher rate of vascular events. OBJECTIVE:The case of essential hypertension is in some ways peculiar: in the past de...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170911102711
更新日期:2017-01-01 00:00:00
abstract::Thymulin is a thymic hormone exclusively produced by the epithelial cells of the thymus. After its discovery and initial characterization in the '70s, it was demonstrated that the production and secretion of thymulin are strongly influenced by the neuro-endocrine system. Conversely, a growing body of evidence, to be r...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666140130211157
更新日期:2014-01-01 00:00:00
abstract::The chemical structure of polyphenols consisting of aromatic rings, capable of quenching free radicals, makes them ideal candidates to protect against oxidation. Polyphenols are present in a variety of foods including grapes, berries, dark chocolate, coffee and tea to mention a few. A number of studies have shown that...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170329144307
更新日期:2017-01-01 00:00:00
abstract::The antifungal agents for systemic mycoses are only a few in number. Among them amphotericin-B is still the most widely used drug, but substantial side effects including nephrotoxicity limits its clinical usefulness. Efforts to lower the toxicity are synthesis of AMPH-B analogues such as AMPH-B esters and encapsulatio...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612023395916
更新日期:2002-01-01 00:00:00
abstract::Human tryptase is a structurally unique and mast cell specific trypsin-like serine protease. Recent biological and immunological investigations have implicated tryptase as a mediator in the pathology of numerous allergic and inflammatory conditions including rhinitis, conjunctivitis, and most notably asthma. A growing...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:
更新日期:1998-10-01 00:00:00
abstract::Release of acetylcholine from parasympathetic nerves in the airways activates postjunctional muscarinic receptors present on smooth muscle, submucosal glands and blood vessels. This triggers bronchoconstriction, muscle hypertrophy, mucus secretion, and vasodilatation, respectively. The release of acetylcholine from pa...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811209023061
更新日期:2012-01-01 00:00:00
abstract:BACKGROUND:Polycystic ovary syndrome (PCOS) is a frequent female reproductive endocrine disease. It has been associated with a number of severe reproductive and metabolic abnormalities. However, there are still open questions especially regarding the best long-term management. METHODS:We summarized the literature focu...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190130104922
更新日期:2018-01-01 00:00:00
abstract::Transfusion-related acute lung injury (TRALI) is a major cause of morbidity and mortality in transfused hosts and like other causes of acute lung injury, there is no effective pharmacologic treatment. The pathophysiology of TRALI is still being defined, but neutrophils have a major role in the pathogenesis of both hum...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612811209023260
更新日期:2012-01-01 00:00:00
abstract::Mass spectrometry information has long offered the potential of discovering biomarkers that would enable clinicians to diagnose disease, and treat it with targeted therapies. PeptideAtlas currently provides access to large-scale spectra data and identification information. This data, and the generation of targeted pep...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/138161212799277833
更新日期:2012-01-01 00:00:00
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
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990434
更新日期:2014-01-01 00:00:00
abstract::Lou Gehrig's disease, a synonym of amyotrophic lateral sclerosis, is an adult-onset lethal neurodegenerative disorder. Irrespective of extensive efforts to elucidate the pathogenesis of the disease and searches for therapies, no favorable pharmacotherapeutic strategies have yet to be proposed. In a popular rodent mode...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666170622105513
更新日期:2017-01-01 00:00:00
abstract:BACKGROUND/OBJECTIVE:KRAS-mutant colorectal cancers (CRC) are tumors that are associated with poor prognosis. However, no effective treatments are available to target them. Therefore, we designed and synthesized novel chalcone analogs, small organic molecules, to investigate their effects on KRAS-mutant CRC cells. MET...
journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826666200206095400
更新日期:2020-01-01 00:00:00
abstract::There is growing evidence for the involvement of glutamatergic abnormalities in schizophrenia. Uncompetitive NMDA receptor (NMDAR) antagonists induce effects closely resembling both the positive and negative symptoms of schizophrenia; candidate risk genes for schizophrenia converge on the NMDAR expressing synapse; and...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161209788957438
更新日期:2009-01-01 00:00:00
abstract:BACKGROUND:Primary aldosteronism is the most common causes of secondary hypertension. Patients suffering from this clinical syndrome have an increased cardiovascular risk and target organ damage. Mineralocorticoid receptor antagonists are the optimal pharmaceutical option for the management of such patients. OBJECTIVE...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666190311130138
更新日期:2018-01-01 00:00:00
abstract::MNPs find numerous important biomedical applications owing to their high biocompatibility and unique magnetic properties at the bottom level. Among several other biomedical applications, MNPs are gaining importance in treating various kinds of cancer either as a hyperthermia agent alone or as a drug/gene carrier for s...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1389203720666190521114936
更新日期:2019-01-01 00:00:00
abstract:BACKGROUND:Cancer causes millions of deaths and huge economic losses every year. The currently practiced methods for cancer therapy have many defects, such as side effects, low curate rate, and discomfort for patients. OBJECTIVE:Herein, we summarize the applications of gold nanorods (AuNRs) in cancer therapy based on ...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612825666191216150052
更新日期:2019-01-01 00:00:00
abstract::The formation of liposomes, nanoparticle micelles, and related systems by mixtures of drugs and/or surfactants is of major relevance for the design of drug delivery systems. We can design new systems using different compounds. Traditionally these systems are created by trial and error using experimental data. However,...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160513150054
更新日期:2016-01-01 00:00:00
abstract::Clopidogrel, in combination wih aspirin, is currently the drug of choice to prevent thrombosis after coronary stent implantation. Currently, clopidogrel is administered to the vast majority of patients without any assessment of platelet inhibition. Response variability and resistance, however, definitely occur to clop...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206776361345
更新日期:2006-01-01 00:00:00
abstract:BACKGROUND:Discovery and development of BCS class 1 drugs through high throughput screening is one of the biggest challenge faced by formulation scientist. METHODS:There are a number of approaches that have been exploited to enhance the solubility and permeability of drugs. Among them, development of nanosuspension ha...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612824666180522100251
更新日期:2018-01-01 00:00:00
abstract::Interest in opioid drugs like morphine, as the oldest and most potent pain-killing agents known, has been maintained through the years. One of the most frequent chronic pain sensations people experience is associated with pathological conditions of the musculoskeletal system. Chronic musculoskeletal pain is a major he...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/13816128113199990363
更新日期:2013-01-01 00:00:00
abstract::Most heterosexual women want to reduce the risk of acquiring a sexually transmitted infection; many also want to control their fertility. Several chemical agents have been proposed to dramatically slow the spread of HIV infections. Ideally, vaginal microbicides, with or without contraceptive properties, should be safe...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161205774580705
更新日期:2005-01-01 00:00:00
abstract::Alcohol dependence is a major disease burden of adults in modern society worldwide. There is no cure for alcohol dependence. In this study, we have examined the molecular targets of ethanol-induced toxicity in humans based on a systematic review of literature data and then discussed current and potential therapeutic t...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210791034030
更新日期:2010-01-01 00:00:00
abstract::Among pediatric patients, preterm neonates and newborns are the most vulnerable subpopulation. Rapid developmental changes of physiological factors affecting the pharmacokinetics of drug substances in newborns require extreme care in dose and dose regimen decisions. These decisions could be supported by in silico meth...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150901110533
更新日期:2015-01-01 00:00:00