Linked Life Data

2863379

Source:http://linkedlifedata.com/resource/pubmed/id/2863379

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
1985-10-17
pubmed:abstractText
Several alpha-adrenoreceptor antagonists were prepared by coupling one of the two moieties of WB 4101 (1) with one of the two moieties of prazosin (2). Their blocking activity and relative selectivity on alpha 1- and alpha 2-adrenoreceptors were evaluated in the isolated rat vas deferens. Although retaining a significant selectivity toward alpha 1-adrenoreceptors, all the drugs were weaker antagonists than the parent compounds 1 and 2. Opening the piperazine ring of 2 gave 3, which displayed a very high activity and selectivity toward alpha 1-adrenoreceptors (alpha 1/alpha 2 = 3890). This may have relevance in understanding the mode of action of prazosin. In addition, 3 may represent a valuable tool in the characterization of alpha-adrenoreceptor subtypes.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0022-2623
pubmed:author
pubmed:issnType
Print
pubmed:volume
28
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1354-7
pubmed:dateRevised
2008-11-21
pubmed:meshHeading
pubmed:year
1985
pubmed:articleTitle
Structure-activity relationships for prazosin and WB 4101 analogues as alpha 1-adrenoreceptor antagonists.
pubmed:publicationType
Journal Article, Comparative Study, Research Support, Non-U.S. Gov't