Premium
Alpha 2A ‐Adrenergic Versus Imidazoline Receptor Controversy in Rilmenidine's Action: Alpha 2A ‐Antagonism in Humans Versus Alpha 2A ‐Agonism in Rabbits
Author(s) -
MOLDERINGS GERHARD J.,
BÖNISCH HEINZ,
BRUSS MICHAEL,
GÖTHERT MANFRED
Publication year - 2003
Publication title -
annals of the new york academy of sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.712
H-Index - 248
eISSN - 1749-6632
pISSN - 0077-8923
DOI - 10.1196/annals.1304.036
Subject(s) - imidazoline receptor , oxymetazoline , alpha (finance) , rilmenidine , alpha 2 adrenergic receptor , antagonism , adrenergic receptor , pharmacodynamics , pharmacology , chemistry , endocrinology , receptor , medicine , adrenergic , agonist , biology , biochemistry , pharmacokinetics , patient satisfaction , construct validity , nursing
A bstract : At the a 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 a 2 ‐adrenoceptor ligands seem to be due to substantial differences in the nucleotide and amino acid sequences between human and rabbit a 2A ‐adrenoceptors. Hence, the rabbit a 2A ‐adrenoceptor is not reliably predictive for the action of ligands at the human a 2A ‐adrenoceptor.