Leukotriene antagonist

Leukotriene antagonist

A leukotriene antagonist is a hormone antagonist acting upon leukotrienes.

It has been demonstrated that leukotrienes are implicated in bronchoconstriction and in the inflammatory cascade leading to asthma. Leukotriene modifiers are an important therapeutic advance in managing asthma.

Approaches

There are two main approaches to block the actions of leukotrienes.

Inhibition of the 5-lipoxygenase pathway

Drugs such as zileuton block 5-lipoxygenase, inhibiting the synthetic pathway of leukotriene metabolism, whereas drugs such as MK-886 block the 5-lipoxygenase activating protein (FLAP) and may help in treating atherosclerosis. [cite journal |author=Jawien J, Gajda M, Rudling M, "et al" |title=Inhibition of five lipoxygenase activating protein (FLAP) by MK-886 decreases atherosclerosis in apoE/LDLR-double knockout mice |journal=Eur. J. Clin. Invest. |volume=36 |issue=3 |pages=141–6 |year=2006 |pmid= |doi=10.1111/j..2006.01606.x |url=http://www.blackwell-synergy.com/doi/abs/10.1111/j..2006.01606.x]

Antagonism of cysteinyl-leukotriene type 1 receptors

Agents such as montelukast and zafirlukast block the actions of cysteinyl leukotrienes at the CysLT1 receptor on target cells such as bronchial smooth muscle.

These modifiers have been shown to improve asthma symptoms, reduce asthma exacerbations and limit markers of inflammation such as eosinophil counts in the peripheral blood and bronchoalveolar lavage fluid. This demonstrates that they have anti-inflammatory properties.

References

External links

*


Wikimedia Foundation. 2010.

Игры ⚽ Поможем написать курсовую

Look at other dictionaries:

  • Leukotriene — Leukotrienes are naturally produced eicosanoid lipid mediators, which may be responsible for the effects of an inflammatory response. Leukotrienes use both autocrine signalling and paracrine signalling to regulate the body s response.… …   Wikipedia

  • Leukotriene B4 receptor — Leukotriene B4 receptor, also known as LTB4R, is a human gene.cite web | title = Entrez Gene: LTB4R leukotriene B4 receptor| url = http://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene Cmd=ShowDetailView TermToSearch=1241| accessdate = ] PBB Summary… …   Wikipedia

  • Antagonist — In biochemistry, an antagonist acts against and blocks an action. For example, insulin lowers the level of glucose (sugar) in the blood, whereas another hormone called glucagon raises it; therefore, insulin and glucagon are antagonists. An… …   Medical dictionary

  • leukotriene receptor antagonist — any of a class of antiasthmatic drugs that bind competitively to leukotriene receptors in the airways, thus inhibiting bronchoconstriction caused by leukotriene mediated inflammatory response …   Medical dictionary

  • leukotriene receptor antagonist — one of a class of drugs that prevent the action of leukotriene by blocking their receptors on cell membranes, such as those in the airways. These drugs are used in the treatment of asthma for their effects in relaxing the smooth muscle of the… …   Medical dictionary

  • leukotriene receptor antagonist — one of a class of drugs that prevent the action of leukotrienes by blocking their receptors on cell membranes, such as those in the airways. These drugs are used in the management of asthma for their effects in relaxing the smooth muscle of the… …   The new mediacal dictionary

  • Cysteinyl leukotriene receptor 1 — Identifiers Symbols CYSLTR1; CYSLT1; CYSLT1R; CYSLTR; HG55; HMTMF81; MGC46139 External IDs …   Wikipedia

  • Cholecystokinin antagonist — A Cholecystokinin antagonist is a specific type of receptor antagonist which blocks the receptor sites for the peptide hormone Cholecystokinin (CCK). There are two subtypes of this receptor known at present, defined as CCKA and CCKB (also called… …   Wikipedia

  • Corticotropin releasing hormone antagonist — A Corticotropin releasing hormone antagonist is a specific type of receptor antagonist which blocks the receptor sites for Corticotropin releasing hormone (also known as Corticotropin releasing factor (CRF)), blocking therefore the consequent… …   Wikipedia

  • LRA (disambiguation) — LRA may refer to: * the Lord s Resistance Army, a rebel group in Uganda * Local Registration Authority, relating to digital keys * Lake Ridge Academy, a school in North Ridgeville, Ohio, USA * Louisiana Recovery Authority, created after the 2005… …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”