Abstract:
:The endothelin family of peptides are extremely potent endogenous vasoconstrictor and pressor agents. Of the 3 isoforms, endothelin-1 is the major isoform produced by the vascular endothelium and is, therefore, likely to be of most importance for regulation of vascular function. Two endothelin receptor subtypes have so far been cloned in mammalian species; ET A, and ET B. Both receptor subtypes are found on smooth muscle cells and mediate the vasoconstrictor and pressor actions of endothelin. The ET B receptor is also found on vascular endothelial cells and mediates endothelin-dependent vasodilatation through release of nitric oxide and prostacyclin. Since their discovery in 1988, the endothelins have been the subject of intense research on their physiological function and potential pathophysiological role in cardiovascular disease. There is now good evidence that endothelin regulates vascular tone and blood pressure, and studies to support the development of endothelin receptor antagonists in conditions associated with chronic vasoconstriction, such as hypertension and heart failure, as well as in vasospastic disorders, such as subarachnoid haemorrhage and Raynaud's disease. There are now a number of selective ET A and combined ET A/B receptor antagonists available for preclinical studies. However, it is still not clear which of these will prove to be of most therapeutic value. Some of these agents are currently being assessed in early phase clinical trials. Endothelin receptor antagonists represent a novel therapeutic approach to a fundamental and newly discovered endogenous vasoconstrictor mechanism. The results of the current clinical trials are awaited with considerable interest.
journal_name
Drugsjournal_title
Drugsauthors
Ferro CJ,Webb DJdoi
10.2165/00003495-199651010-00003subject
Has Abstractpub_date
1996-01-01 00:00:00pages
12-27issue
1eissn
0012-6667issn
1179-1950journal_volume
51pub_type
杂志文章,评审相关文献
DRUGS文献大全abstract::Acamprosate (Campral(®), Aotal(®), Regtect(®)) is one of a limited number of pharmacological treatment options approved as an adjunct to psychosocial interventions to facilitate the maintenance of abstinence in alcohol-dependent patients. It has been used in Europe, the USA and other countries for many years and was r...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-015-0423-9
更新日期:2015-07-01 00:00:00
abstract::The number of effective cytotoxic agents for the treatment of patients with metastatic adult soft tissue sarcoma is limited, especially when patients have failed anthracycline- and ifosfamide-based chemotherapy. For the subgroup of patients with inoperable gastrointestinal stromal tumour (GIST), progress has been made...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200565020-00002
更新日期:2005-01-01 00:00:00
abstract::Bisoprolol is a beta 1-adrenoceptor antagonist with no partial agonist (intrinsic sympathomimetic) activity or membrane stabilising (local anaesthetic) activity. The oral bioavailability of bisoprolol is high (90%) and the drug has a long elimination half-life which allows once-daily administration; in addition, it is...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198836030-00002
更新日期:1988-09-01 00:00:00
abstract::Page 9, Fig. 2, which originally appeared as. ...
journal_title:Drugs
pub_type: 已发布勘误
doi:10.1007/s40265-020-01416-7
更新日期:2020-10-01 00:00:00
abstract::The new therapeutic options available to clinicians treating dyslipidaemia in the last decade have enabled effective treatment for many patients. The development of the HMG-CoA reductase inhibitors (statins) have been a major advance in that they possess multiple pharmacological effects (pleiotropic effects) resulting...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200060010-00005
更新日期:2000-07-01 00:00:00
abstract::The successful identification of a range of leukaemia-specific and lymphoma-specific antigens in recent years has stimulated efforts to develop therapeutic vaccination strategies. A number of clinical trials have established the safety and immunogenicity of vaccination against tumour antigens, although there are limit...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/11593270-000000000-00000
更新日期:2011-09-10 00:00:00
abstract::Information about the value for money of a medicine as derived from an economic evaluation can be used for decision-making purposes by policy makers, healthcare payers, healthcare professionals and pharmaceutical companies. This article illustrates the use of economic evaluation by decision makers and formulates a num...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/11538120-000000000-00000
更新日期:2010-10-22 00:00:00
abstract::Subcutaneous dulaglutide (Trulicity®) is a once-weekly glucagon-like peptide-1 receptor agonist that is approved in numerous countries as an adjunct to diet and exercise for the treatment of adults with type 2 diabetes (T2D). In the clinical trial and real-world settings, once-weekly subcutaneous dulaglutide, as monot...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-020-01260-9
更新日期:2020-02-01 00:00:00
abstract::Lanreotide Autogel (ATG) [Somatuline Depot] is a novel, long-acting preparation of the somatostatin analogue lanreotide acetate that acts via somatostatin receptors to reduce both growth hormone (GH) and insulin-like growth factor-I (IGF-I) levels. It is indicated for the management of acromegaly and, relative to most...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200868050-00013
更新日期:2008-01-01 00:00:00
abstract:UNLABELLED:Dofetilide is a 'pure' class III antiarrhythmic agent which has demonstrated efficacy in the conversion of atrial fibrillation or flutter to sinus rhythm and the maintenance of sinus rhythm. By blocking the rapid component of the cardiac delayed rectifier potassium current (I(Kr)), dofetilide prolongs the ca...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199958060-00007
更新日期:1999-12-01 00:00:00
abstract::Antibacterial activities of cefotaxime and its major metabolite, desacetylcefotaxime, against 178 strains (of 10 species) were assessed in terms of minimum inhibitory concentrations (MIC50 and MIC80), and were compared with those of cefoperazone and ceftazidime. The activity of desacetylcefotaxime was several times le...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/00003495-198800352-00013
更新日期:1988-01-01 00:00:00
abstract::Endothelial dysfunction and increased arterial stiffness occur early in the pathogenesis of diabetic vasculopathy. They are both powerful independent predictors of cardiovascular risk. Advances in non-invasive methodologies have led to widespread clinical investigation of these abnormalities in diabetes mellitus, gene...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200565010-00003
更新日期:2005-01-01 00:00:00
abstract::Oral abiraterone acetate, in combination with prednisone/prednisolone, is used to treat patients with metastatic castration-resistant prostate cancer (CRPC) who have previously received docetaxel-containing chemotherapy. Abiraterone acetate was developed to specifically inhibit cytochrome P450 (CYP)17A1, which is an e...
journal_title:Drugs
pub_type: 杂志文章
doi:10.2165/11208080-000000000-00000
更新日期:2011-10-22 00:00:00
abstract::Vildagliptin (Galvus) is an antihyperglycaemic agent that selectively inhibits the dipeptidyl peptidase-4 (DPP-4) enzyme. Such inhibition prevents the degradation of the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). This results in improved glycaemic control ...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/0003495-200868160-00009
更新日期:2008-01-01 00:00:00
abstract::In a double-blind study, the efficacy and tolerability of nimesulide (100mg twice daily) were compared with those of diclofenac (50mg twice daily) when administered orally to 50 patients with acute superficial thrombophlebitis of the lower limbs. Pain relief and amelioration of inflammation were apparent in patients t...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-199300461-00050
更新日期:1993-01-01 00:00:00
abstract:UNLABELLED:Zolpidem is an imidazopyridine agent that is indicated for the short term (< or = 4 weeks) treatment of insomnia (recommended dosage 10 mg/day in adults and 5 or 10 mg/day in the elderly or patients with hepatic impairment). Data have shown that the hypnotic efficacy of zolpidem is generally comparable to th...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200059040-00014
更新日期:2000-04-01 00:00:00
abstract::General anaesthesia is the reversible depression of central nervous system function. There is still no agreement over what constitutes depth of anaesthesia, and the clinical anaesthetist must thus titrate drug input according to clinical signs (heart rate, blood pressure, somatic movement, autonomic responses). The po...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199243010-00006
更新日期:1992-01-01 00:00:00
abstract::Non-insulin-dependent diabetes mellitus (NIDDM, type 2 diabetes) is a heterogeneous disease resulting from a dynamic interaction between defects in insulin secretion and insulin action. There are various pharmacological approaches to improving glucose homeostasis, but those currently used in clinical practice either d...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199754030-00001
更新日期:1997-09-01 00:00:00
abstract::This review will discuss the safety profiles of the angiotensin-converting enzyme (ACE) inhibitors captopril, enalapril and lisinopril in patients with hypertension. In general, the safety profiles of ACE inhibitors compare favourably with those of other agents used for the treatment of hypertension. Adverse effects a...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198800355-00016
更新日期:1988-01-01 00:00:00
abstract::Enasidenib (Idhifa®) is an oral isocitrate dehydrogenase-2 (IDH2) inhibitor developed by Celgene Corporation under a global, exclusive license from Agios Pharmaceuticals. Enasidenib has been approved in the USA for the treatment of adults with relapsed or refractory acute myeloid leukaemia (AML) and an IDH2 mutation a...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-017-0813-2
更新日期:2017-10-01 00:00:00
abstract::Rabeprazole is an inhibitor of the gastric proton pump. It causes dose-dependent inhibition of acid secretion and has a more rapid onset of action than omeprazole. Duodenal ulcers healed faster after treatment with rabeprazole 20 or 40 mg/day than placebo or ranitidine 150 mg 4 times daily and at a generally similar r...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199958040-00014
更新日期:1999-10-01 00:00:00
abstract::Cenobamate (XCOPRI®) is an oral, small molecule neurotherapeutic azole compound that is being developed by SK Life Science Inc. and Arvelle Therapeutics for the treatment of epilepsy. Based on results of two pivotal phase 2 trials, cenobamate was recently approved in the USA for use in the treatment of partial-onset s...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.1007/s40265-019-01250-6
更新日期:2020-01-01 00:00:00
abstract::Pregabalin, the pharmacologically active S-enantiomer of 3-aminomethyl-5-methyl-hexanoic acid, has a similar pharmacological profile to that of its developmental predecessor gabapentin, but showed greater analgesic activity in rodent models of neuropathic pain. The exact mechanism of action of pregabalin is unclear, a...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200464240-00006
更新日期:2004-01-01 00:00:00
abstract::Meloxicam is a new nonsteroidal anti-inflammatory drug (NSAID) developed for the treatment of rheumatoid arthritis and osteoarthritis. It has greater in vitro and in vivo inhibitory action against the inducible isoform of cyclo-oxygenase (COX-2), which is implicated in the inflammatory response, than against the const...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199651030-00007
更新日期:1996-03-01 00:00:00
abstract::Hepatitis C virus (HCV) infection is associated with a variable disease course and response to therapy. Some infected patients may develop little or no disease for 30 to 40 years, whereas others will develop cirrhosis within 5 to 10 years. Both host and viral factors influence the rate of disease progression. The mana...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199600522-00003
更新日期:1996-01-01 00:00:00
abstract::During the 40 years since the initial synthesis of fluorouracil, there have been many attempts to improve fluoropyrimidine chemotherapy. These have included the utilisation of different schedules of fluorouracil administration, modulation of the metabolism of fluorouracil with other drugs to increase its therapeutic b...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-199958003-00016
更新日期:1999-01-01 00:00:00
abstract::A somatropin preparation (Zorbtive) produced by recombinant DNA technology has been evaluated in patients with short bowel syndrome. Somatropin is thought to enhance intestinal adaptation in this condition through direct or indirect effects on the intestine. In a randomised, double-blind study in patients with short b...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-200464120-00008
更新日期:2004-01-01 00:00:00
abstract::A number of drugs are available that act fairly specifically as "mild" analgesics, although this description by no means implies that their clinical effectiveness is limited to the relief of slight pain and trivial disability. They are effective by mouth and their action is mediated peripherally. Among the possible me...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-197510050-00007
更新日期:1975-01-01 00:00:00
abstract:UNLABELLED:Joint pain is the main complaint in patients affected by osteoarthritis (OA), and NSAIDs are commonly used to treat pain associated with OA. Over the past few years, cyclo-oxygenase (COX)-2-selective inhibitors have been proved to have certain advantages over non-selective NSAIDs and have been increasingly u...
journal_title:Drugs
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.2165/00003495-200363001-00006
更新日期:2003-01-01 00:00:00
abstract::Slowing of nerve conduction, a hallmark of both experimental and human diabetic neuropathy, is improved or corrected by aldose reductase inhibitors such as sorbinil. Animal experiments suggest that a myo-inositol-related defect in nerve sodium-potassium adenosine triphosphatase (ATPase) is responsible for the acute re...
journal_title:Drugs
pub_type: 杂志文章,评审
doi:10.2165/00003495-198600322-00004
更新日期:1986-01-01 00:00:00