The clinical potential of endothelin receptor antagonists in cardiovascular medicine.

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

Drugs

journal_title

Drugs

authors

Ferro CJ,Webb DJ

doi

10.2165/00003495-199651010-00003

subject

Has Abstract

pub_date

1996-01-01 00:00:00

pages

12-27

issue

1

eissn

0012-6667

issn

1179-1950

journal_volume

51

pub_type

杂志文章,评审

相关文献

DRUGS文献大全
  • Acamprosate: A Review of Its Use in Alcohol Dependence.

    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

    authors: Plosker GL

    更新日期:2015-07-01 00:00:00

  • Recent developments in salvage chemotherapy for patients with metastatic soft tissue sarcoma.

    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

    authors: Hartmann JT,Patel S

    更新日期:2005-01-01 00:00:00

  • Bisoprolol. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in hypertension and angina pectoris.

    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

    authors: Lancaster SG,Sorkin EM

    更新日期:1988-09-01 00:00:00

  • Correction to: Deprescribing Opioids in Chronic Non‑cancer Pain: Systematic Review of Randomised Trials.

    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

    authors: Mathieson S,Maher CG,Ferreira GE,Hamilton M,Jansen J,McLachlan AJ,Underwood M,Lin CC

    更新日期:2020-10-01 00:00:00

  • Current, new and future treatments in dyslipidaemia and atherosclerosis.

    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

    authors: Chong PH,Bachenheimer BS

    更新日期:2000-07-01 00:00:00

  • Vaccination strategies in lymphomas and leukaemias: recent progress.

    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

    authors: Rezvani K,de Lavallade H

    更新日期:2011-09-10 00:00:00

  • Use of economic evaluation in decision making: evidence and recommendations for improvement.

    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

    authors: Simoens S

    更新日期:2010-10-22 00:00:00

  • Dulaglutide: A Review in Type 2 Diabetes.

    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

    authors: Scott LJ

    更新日期:2020-02-01 00:00:00

  • Lanreotide Autogel: a review of its use in the management of acromegaly.

    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

    authors: Croxtall JD,Scott LJ

    更新日期:2008-01-01 00:00:00

  • Dofetilide: a review of its use in atrial fibrillation and atrial flutter.

    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

    authors: McClellan KJ,Markham A

    更新日期:1999-12-01 00:00:00

  • In vitro activity of desacetylcefotaxime and the interaction with its parent compound, cefotaxime.

    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

    authors: Oizumi K,Hayashi I,Aonuma S,Konno K

    更新日期:1988-01-01 00:00:00

  • Mechanisms, significance and treatment of vascular dysfunction in type 2 diabetes mellitus: focus on lipid-regulating therapy.

    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

    authors: Woodman RJ,Chew GT,Watts GF

    更新日期:2005-01-01 00:00:00

  • Abiraterone acetate: in metastatic castration-resistant prostate cancer.

    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

    authors: Yang LP

    更新日期:2011-10-22 00:00:00

  • Vildagliptin: a review of its use in the management of type 2 diabetes mellitus.

    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

    authors: Croxtall JD,Keam SJ

    更新日期:2008-01-01 00:00:00

  • A comparison of nimesulide and diclofenac in the treatment of acute superficial thrombophlebitis.

    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

    authors: Ferrari E,Pratesi C,Scaricabarozzi I

    更新日期:1993-01-01 00:00:00

  • Zolpidem: an update of its pharmacology, therapeutic efficacy and tolerability in the treatment of insomnia.

    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

    authors: Holm KJ,Goa KL

    更新日期:2000-04-01 00:00:00

  • Practical treatment recommendations for the safe use of anaesthetics.

    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

    authors: Sear JW

    更新日期:1992-01-01 00:00:00

  • Drug treatment of non-insulin-dependent diabetes mellitus in the 1990s. Achievements and future developments.

    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

    authors: Scheen AJ

    更新日期:1997-09-01 00:00:00

  • Safety profiles of the angiotensin-converting enzyme inhibitors.

    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

    authors: Warner NJ,Rush JE

    更新日期:1988-01-01 00:00:00

  • Enasidenib: First Global Approval.

    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

    authors: Kim ES

    更新日期:2017-10-01 00:00:00

  • Rabeprazole: a review of its use in acid-related gastrointestinal disorders.

    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

    authors: Langtry HD,Markham A

    更新日期:1999-10-01 00:00:00

  • Cenobamate: First Approval.

    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

    authors: Keam SJ

    更新日期:2020-01-01 00:00:00

  • Pregabalin: in the treatment of painful diabetic peripheral neuropathy.

    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

    authors: Frampton JE,Scott LJ

    更新日期:2004-01-01 00:00:00

  • Meloxicam.

    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

    authors: Noble S,Balfour JA

    更新日期:1996-03-01 00:00:00

  • Pathophysiology and treatment of hepatitis C.

    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

    authors: Thomas HC,Booth J,Brown J

    更新日期:1996-01-01 00:00:00

  • Improving fluorouracil chemotherapy with novel orally administered fluoropyrimidines.

    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

    authors: Diasio RB

    更新日期:1999-01-01 00:00:00

  • Somatropin (Zorbtive): in short bowel syndrome.

    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

    authors: Keating GM,Wellington K

    更新日期:2004-01-01 00:00:00

  • Simple analgesics.

    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

    authors: Parkhouse J

    更新日期:1975-01-01 00:00:00

  • A randomised, double-blind, clinical trial comparing the efficacy of nimesulide, celecoxib and rofecoxib in osteoarthritis of the knee.

    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

    authors: Bianchi M,Broggini M

    更新日期:2003-01-01 00:00:00

  • Sorbitol, myo-inositol and sodium-potassium ATPase in diabetic peripheral nerve.

    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

    authors: Greene DA

    更新日期:1986-01-01 00:00:00