Alpha 2A ‐Adrenergic Versus Imidazoline Receptor Controversy in Rilmenidine's Action: Alpha 2A ‐Antagonism in Humans Versus Alpha 2A ‐Agonism in Rabbits | Zendy

MOLDERINGS GERHARD J. | Zendy; BÖNISCH HEINZ | Zendy; BRUSS MICHAEL | Zendy; GÖTHERT MANFRED | Zendy

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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.

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