Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6 Pt 2
pubmed:dateCreated
1998-7-9
pubmed:abstractText
Preclinical pharmacological studies have demonstrated that cysLT, receptor antagonists, such as zafirlukast, montelukast, and pobilukast, are potent and selective antagonists of cysteinyl leukotriene (cysLT) activity. In vitro, these agents compete with [3H]LTD4 for binding to cysLT, receptors present on guinea pig and human lung cell membranes. Both zafirlukast and montelukast have affinities that are approximately two times greater than that of the natural ligand, LTD4. These agents block LTD4- and LTE4-induced contractions of isolated guinea pig trachea, but do not antagonize LTC4-induced contractions, which are putatively mediated by a different LT receptor, cysLT2. The cysLT2 receptor, however, has not yet been found in human airway smooth muscle. In animal models, these drugs inhibit LTD4-, LTE4-, and antigen-induced bronchoconstriction, reduce inflammatory markers in models of pulmonary inflammation, and inhibit antigen-induced late-phase bronchoconstriction. This preclinical profile suggests that cysLT, receptor antagonists may be useful in treating inflammatory conditions of the respiratory system, such as asthma and allergic rhinitis.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
AIM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
1073-449X
pubmed:author
pubmed:issnType
Print
pubmed:volume
157
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
S214-8; discussion S218-9, S247-8
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1998
pubmed:articleTitle
Pharmacology of leukotriene receptor antagonists.
pubmed:affiliation
Zeneca Pharmaceutical, Wilmington, Delaware 19897, USA. David.Aharony@phwilm.zeneca.com
pubmed:publicationType
Journal Article, In Vitro, Review