Linked Life Data

1685186

Source:http://linkedlifedata.com/resource/pubmed/id/1685186

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
5
pubmed:dateCreated
1992-2-24
pubmed:abstractText
Using a radioligand binding assay, we assessed the affinity and selectivity of the antagonistic effects of bopindolol (4-(benzoyloxy-3-tert-butylaminopropyl)-2-methylindole hydrogen-malonate) and its two metabolites, (18-502, (4-(3-tert-butylamino-2-hydroxypropoxy)-2-methyl indole) and 20-785, (4-(3-tert-butylaminopropoxy)-2-carboxyl indole], for beta 1- and beta 2-adrenoceptors and on 5HT1B-receptors in rat brain and heart. In addition, we also determined the pA2 values of these agents for their antagonistic effects toward positive chronotropic and inotropic actions (beta 1-adrenoceptors) and for their antagonistic effects toward isolated tracheal relaxation (beta 2-adrenoceptors), using isoproterenol as an agonist. The data showed that bopindolol was more selective for beta 2-adrenoceptors than for beta 1-adrenoceptors and 5HT1B-receptors, but its two metabolites (18-502 and 20-785) did not have significant selectivity for beta 1- and beta 2-adrenoceptors, using both [3H]CGP12177 and [125I]ICYP ([125I]iodocyanopindolol) bindings. In contrast, the results from pharmacological assessment for antagonistic potencies, using atria and trachea, showed that bopindolol and its two metabolites did not have significant selectivity on beta 1- and beta 2-adrenoceptors. A major metabolite of bopindolol, 18-502, had higher pKi and pA2 values for beta-adrenoceptors and 5HT1B-receptors than those of bopindolol and 20-785. These results indicate, first, that a radioligand binding assay for the assessment of the selectivity of bopindolol and its two metabolites for beta 1- and beta 2-adrenoceptors is more effective than pharmacological experiments, and that there is a possibility that its two metabolites also contribute to the strong beta-blocking action of bopindolol.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
May
pubmed:issn
0386-846X
pubmed:author
pubmed:issnType
Print
pubmed:volume
14
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
250-5
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
1991
pubmed:articleTitle
Beta-blocking potency and selectivity of bopindolol and its two metabolites for beta 1- and beta 2-adrenergic receptors as assessed by radioligand binding assay.
pubmed:affiliation
Department of Pharmacology, Niigata College of Pharmacy, Japan.
pubmed:publicationType
Journal Article, In Vitro