Linked Life Data

3398002

Source:http://linkedlifedata.com/resource/pubmed/id/3398002

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
8
pubmed:dateCreated
1988-9-2
pubmed:abstractText
The "inactive metabolite approach" was used to design a series of "soft" drugs derived from the acidic metabolite of metoprolol. Pharmacokinetic and pharmacodynamic properties of these novel "soft" beta-adrenoceptor antagonists were determined: half-lives in human blood ranged from 5 to 754 min. The rates of in vivo disappearance of representative slow, medium, and fast hydrolyzing esters were determined in rats. In each case rapid and quantitative conversion to the corresponding free acid was observed. This suggests a facile, one-step degradation to the predicted major metabolite. The compounds were tested for their ability to decrease intraocular pressure in a rabbit model. Five of the new compounds exerted an ocular hypotensive action comparable to or greater than that of the reference compound, timolol maleate, and with a prolonged duration of action in some cases. In contrast the new compounds showed reduced and shorter duration systemic activity. The adamantylethyl ester emerges as a potentially effective antiglaucoma agent with significantly improved site-specific activity.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
31
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1651-6
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1988
pubmed:articleTitle
Soft drugs. 7. Soft beta-blockers for systemic and ophthalmic use.
pubmed:affiliation
University of Florida, College of Pharmacy, Center for Drug Design and Delivery, J. Hillis Miller Health Center, Gainesville 32610.
pubmed:publicationType
Journal Article, In Vitro