Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
3
pubmed:dateCreated
1987-7-30
pubmed:abstractText
The selective beta-2 adrenoceptor agonist procaterol produced positive inotropic and chronotropic responses over a concentration range of 1 nM to 0.1 mM in spontaneously beating right atria and in three of seven electrically driven left atria. The pD2 values (right atria, 7.30; left atria, 7.18) were midway between its known affinities at beta-1 and beta-2 adrenoceptors and are evidence that positive inotropic and chronotropic responses involve a minor beta-2 adrenoceptor component. The pKB values for procaterol against (-)-isoproterenol in the right atria (5.59) and left atria (5.29) were consistent with its affinity for beta-1 adrenoceptors and suggest that these are responsible primarily for positive inotropic and chronotropic responses. Receptor binding studies in right atrial homogenates showed that [125I]cyanopindolol binding was saturable (KD = 36.2 pM, maximal density of binding sites = 49.2 fmol mg-1 protein) and stereoselective with respect to the isomers of propranolol. Competition binding curves for the beta-1 adrenoceptor antagonist CGP 20712A and beta-2 selective antagonist ICI 118,551 against [125I]cyanopindolol binding were resolved into two components using iterative curve fitting techniques. Binding sites with the characteristics of beta-1 and beta-2 adrenoceptors were present in the proportions of approximately 75 to 25%. These studies indicate either that the beta-1 adrenoceptor is coupled more efficiently to the positive inotropic and chronotropic response than the beta-2 adrenoceptor or that a proportion of the beta-2 adrenoceptors subserve other functions.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Jun
pubmed:issn
0022-3565
pubmed:author
pubmed:issnType
Print
pubmed:volume
241
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
1041-7
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1987
pubmed:articleTitle
Characterization of beta-1 and beta-2 adrenoceptors in guinea pig atrium: functional and receptor binding studies.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't