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

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

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...

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Veröffentlicht in:Annals of the New York Academy of Sciences 2003-12, Vol.1009, p.279-282
Hauptverfasser: Molderings, Gerhard J, Bonisch, Heinz, Bruss, Michael, Gothert, Manfred
Format: Artikel
Sprache:eng
Schlagworte:
Adrenergic alpha-Agonists - metabolism
Adrenergic alpha-Agonists - pharmacology
Adrenergic alpha-Antagonists - metabolism
Adrenergic alpha-Antagonists - pharmacology
Amino Acid Sequence
Animals
Antihypertensive Agents - metabolism
Antihypertensive Agents - pharmacology
Humans
Imidazoline Receptors
Molecular Sequence Data
Oxazoles - metabolism
Oxazoles - pharmacology
Oxymetazoline - metabolism
Oxymetazoline - pharmacology
Rabbits
Receptors, Adrenergic, alpha-2 - chemistry
Receptors, Adrenergic, alpha-2 - genetics
Receptors, Adrenergic, alpha-2 - metabolism
Receptors, Drug - metabolism
Rilmenidine
Sequence Alignment
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Zusammenfassung: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.
ISSN:0077-8923