Alpha(2A)-adrenergic versus imidazoline receptor controversy in rilmenidine's action: alpha(2A)-antagonism in humans versus alpha(2A)-agonism in rabbits.

Abstract:

:At the alpha(2A)-autoreceptors on the sympathetic nerve terminals of the human atrial appendages and rabbit pulmonary artery, rilmenidine and oxymetazoline exhibit different properties (antagonism and agonism, respectively). These opposite pharmacodynamic properties of alpha(2)-adrenoceptor ligands seem to be due to substantial differences in the nucleotide and amino acid sequences between human and rabbit alpha(2A)-adrenoceptors. Hence, the rabbit alpha(2A)-adrenoceptor is not reliably predictive for the action of ligands at the human alpha(2A)-adrenoceptor.

journal_name

Ann N Y Acad Sci

authors

Molderings GJ,Bonisch H,Bruss M,Gothert M

doi

10.1196/annals.1304.036

subject

Has Abstract

pub_date

2003-12-01 00:00:00

pages

279-82

eissn

0077-8923

issn

1749-6632

journal_volume

1009

pub_type

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