Linked Life Data

8315513

Source:http://linkedlifedata.com/resource/pubmed/id/8315513

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1993-7-29
pubmed:abstractText
DISCOVERY OF LOSARTAN: Losartan (DuP 753, MK 954) is the first potent and selective non-peptide angiotensin II (Ang II) antagonist. The discovery of losartan followed an observation that several simple benzylimidazoles are weak Ang II antagonists. These compounds (e.g. S8307) lack potency but are orally active and selective for Ang II receptors (AT receptors). Losartan was synthesized using S8307 and other analogs of the benzylimidazoles as chemical leads. ACTION OF LOSARTAN: Losartan selectively inhibits all Ang II responses that have been studied and lowers blood pressure in several animal models of renin-dependent hypertension. In animals, the antihypertensive efficacy of losartan is similar to that of angiotensin converting enzyme (ACE) inhibitors but, unlike ACE inhibitors, losartan is a more selective inhibitor of the renin-angiotensin system since it does not affect the metabolism of kinins. Compared with peptide Ang II antagonists (e.g. saralasin), losartan has significant advantages, including a long duration of action, effective oral absorption and no Ang II agonist activity. CONCLUSIONS: The high selectivity and potency for AT receptors, the non-peptide structure and the oral activity of losartan represent a pharmacological breakthrough. This agent is now being used to elucidate the physiology of AT receptors and is likely to be useful in the therapeutic management of diseases in which the renin-angiotensin system is known to be involved.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Apr
pubmed:issn
0952-1178
pubmed:author
pubmed:issnType
Print
pubmed:volume
11
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
S19-22
pubmed:dateRevised
2011-1-11
pubmed:meshHeading
pubmed:year
1993
pubmed:articleTitle
Discovery of losartan, the first specific non-peptide angiotensin II receptor antagonist.
pubmed:affiliation
Merck Research Laboratories, West Point, PA 19486.
pubmed:publicationType
Journal Article, Review