Linked Life Data

1666366

Source:http://linkedlifedata.com/resource/pubmed/id/1666366

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
2
pubmed:dateCreated
1992-4-28
pubmed:abstractText
We developed a method for the simultaneous determination of drug affinity constants for rat alpha 2A- and alpha 2B-adrenoceptor subtypes by using [3H]RX821002 radioligand binding in the kidney. Three competition curves were obtained for each drug: one for the test compound in the absence of ARC 239 (a drug found to have 108-fold higher affinity for alpha 2B- than for alpha 2A-adrenoceptors), one in the presence of ARC 239, and one for ARC 239. It is possible to determine the Kds of a tested drug for both alpha 2A- and alpha 2B-adrenoceptors by simultaneous computer modelling because of the increased constraint in the calculations given by the inclusion of ARC 239 into the assay. Using this approach, we found guanfacine and oxymetazoline to be highly alpha 2A-selective. The most alpha 2B-selective were ARC 239, prazosin and corynanthine. A number of other drugs, for example UK-14,304, rilmenidine and clonidine, were non-selective or showed minor selectivity for alpha 2A- or alpha 2B-adrenoceptors. Moreover, using Monte Carlo simulations, we showed that the three-curve method gives more accurate estimates of drug binding constants for assays when two receptor sites are present than methods analysing only one competition curve.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Sep
pubmed:issn
0014-2999
pubmed:author
pubmed:issnType
Print
pubmed:day
17
pubmed:volume
202
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
235-43
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Delineation of rat kidney alpha 2A- and alpha 2B-adrenoceptors with [3H]RX821002 radioligand binding: computer modelling reveals that guanfacine is an alpha 2A-selective compound.
pubmed:affiliation
Department of Pharmacology, Umeå University, Sweden.
pubmed:publicationType
Journal Article, In Vitro, Research Support, Non-U.S. Gov't