Linked Life Data

9354232

Source:http://linkedlifedata.com/resource/pubmed/id/9354232

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
9
pubmed:dateCreated
1997-12-19
pubmed:abstractText
The enantiomers of benzyl-(2-chloroethyl)-[2-(2-methoxyphenoxy) -1-methylethyl]amine hydrochloride (1, CM18) were synthesized and studied pharmacologically for their irreversible antagonism at rat vas deferens alpha-adrenoceptors. In addition, assignment of the absolute configuration of the two enantiomers of 1 was made by X-ray crystallographic analysis performed on the intermediate amine (+)-2 hydrochloride. The enantiomer (R)-(+)-1 [(R)-(+)-CM18] (a) had a 10-fold preferential blocking activity for alpha 1-versus alpha 2-adrenoceptors, (b) discriminated, like racemic 1, between two possible alpha 1-adrenoceptor subsites/subtypes, with a selectivity ratio of 6.5 and (c) was 10-23 times as potent as the (S)-(-)-enantiomer at alpha 2- and alpha 1-adrenoceptors. Thus, it may be a valuable tool for the characterization of rat vas deferens alpha 1-adrenoceptor subtypes.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0968-0896
pubmed:author
pubmed:issnType
Print
pubmed:volume
5
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1775-82
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1997
pubmed:articleTitle
Synthesis and alpha-adrenoceptor blocking activity of the enantiomers of benzyl-(2-chloroethyl)-[2-(2-methoxyphenoxy)-1-methylethyl]amine hydrochloride.
pubmed:affiliation
Department of Chemical Sciences, University of Camerino, Italy. giardina@camserv.unicam.it
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't