Comparison of [3H]tamsulosin and [3H]prazosin binding to wild-type and constitutively active alpha1B-adrenoceptors.

Détails

ID Serval
serval:BIB_6B21144E0008
Type
Article: article d'un périodique ou d'un magazine.
Collection
Publications
Titre
Comparison of [3H]tamsulosin and [3H]prazosin binding to wild-type and constitutively active alpha1B-adrenoceptors.
Périodique
Life Sciences
Auteur(s)
Hein P., Goepel M., Cotecchia S., Michel M.C.
ISSN
0024-3205 (Print)
ISSN-L
0024-3205
Statut éditorial
Publié
Date de publication
2000
Volume
67
Numéro
5
Pages
503-508
Langue
anglais
Résumé
We have tested the hypothesis that smaller alpha1B-adrenoceptor labeling by [3H]tamsulosin compared to [3H]prazosin is related to differential recognition of agonist low affinity states. Paired saturation binding experiments with [3H]prazosin and [3H]tamsulosin were performed in membrane preparations from rat liver and Rat- fibroblasts stably transfected with wild-type hamster alpha1B-adrenoceptors or a constitutively active mutant thereof. In all three settings [3H]tamsulosin labeled significantly fewer alpha1B-adrenoceptors than [3H]prazosin. In noradrenaline competition binding experiments, the percentage of agonist low affinity sites was smallest for the constitutively active alpha1B-adrenoceptor but the percentage of agonist low affinity sites recognized by [3H]tamsulosin and [3H]prazosin did not differ significantly. We conclude that [3H]tamsulosin labels fewer alpha1B-adrenoceptors than [3H]prazosin but this is not fully explained by a poorer labeling of agonist low affinity sites.
Mots-clé
Adrenergic alpha-Antagonists/metabolism, Animals, Cricetinae, Male, Prazosin/metabolism, Radioligand Assay, Rats, Rats, Wistar, Receptors, Adrenergic, alpha-1/metabolism, Sulfonamides/metabolism, Tritium
Pubmed
Web of science
Création de la notice
24/01/2008 11:05
Dernière modification de la notice
20/08/2019 14:25
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