Linked Life Data

6311586

Source:http://linkedlifedata.com/resource/pubmed/id/6311586

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
4
pubmed:dateCreated
1983-11-23
pubmed:abstractText
The affinities of several ergot derivatives for rat cerebral cortex alpha 1- and alpha 2-adrenoceptors were assessed using radioligand binding techniques. In most cases both [3H]prazosin (labelling alpha 1-adrenoceptors) and [3H]rauwolscine (labelling alpha 2-adrenoceptors) binding were displaced by the ergot derivatives tested, but with markedly different potency. Generally compounds displayed selectivity toward the alpha 2-adrenoceptor, particularly CQ 32-084, which had a Ki value against [3H]rauwolscine binding of 35 nM, but had little effect on [3H]prazosin binding at concentrations in excess of 5 microM. Lisuride was the most potent displacer of [3H]rauwolscine binding with a Ki value of 0.54 nM. Only bromocriptine was relatively alpha 1-selective with a Ki against [3H]prazosin binding of 18 nM and against [3H]rauwolscine binding of 120 nM. The results indicate that the ergot derivatives tested display a marked affinity for alpha-adrenoceptors and that their actions at this receptor class should be considered when interpreting their pharmacological activity in vivo.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Aug
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
5
pubmed:volume
91
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
363-9
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1983
pubmed:articleTitle
The selectivity of some ergot derivatives for alpha 1 and alpha 2-adrenoceptors of rat cerebral cortex.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't