Moxonidine Displays a Presynaptic Alpha-2-Adrenoceptor-Dependent Synergistic Sympathoinhibitory Action at Imidazoline-1 Receptors

: The function of presynaptic imidazoline‐1 receptors (I1‐R) in the heart remains unclear. In rat hearts, UK14.304 and moxonidine reduced norepinephrine (NE) release. AGN192403 had no influence on NE, whereas rilmenidine, agmatine, rauwolscine, and efaroxan increased NE. These effects of moxonidine...

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Bibliographic Details
Published in:Annals of the New York Academy of Sciences 2003-12, Vol.1009 (1), p.265-269
Main Authors: SCHÄFER, ULRICH, BURGDORF, CHRISTOF, ENGELHARDT, ASTRID, RAASCH, WALTER, KURZ, THOMAS, RICHARDT, GERT
Format: Article
Language:English
Subjects:
Adrenergic alpha-Agonists - pharmacology
Adrenergic alpha-Antagonists - pharmacology
Agmatine - pharmacology
alpha-2-adrenoceptor
Animals
Benzofurans - pharmacology
Bridged Bicyclo Compounds - pharmacology
Brimonidine Tartrate
Drug Synergism
Heart - drug effects
Heart - physiology
Heptanes - pharmacology
Imidazoles - pharmacology
Imidazoline Receptors
imidazoline-1-receptor
moxonidine
Norepinephrine - metabolism
Oxazoles - pharmacology
Quinoxalines - pharmacology
Rats
Rats, Wistar
Receptors, Adrenergic, alpha-2 - metabolism
Receptors, Drug - metabolism
Rilmenidine
Sympathetic Nervous System - drug effects
Sympathetic Nervous System - physiology
Sympatholytics - pharmacology
synergistic action
Yohimbine - pharmacology
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Summary:: The function of presynaptic imidazoline‐1 receptors (I1‐R) in the heart remains unclear. In rat hearts, UK14.304 and moxonidine reduced norepinephrine (NE) release. AGN192403 had no influence on NE, whereas rilmenidine, agmatine, rauwolscine, and efaroxan increased NE. These effects of moxonidine and rilmenidine were not affected by AGN192403 adminstration. Conversely, after pretreatment with UK14.304, only moxonidine displayed a pronounced inhibitory action on NE release (sensitive to AGN192403), indicating a synergistic inhibitory action at I1‐R under conditions of a stimulated alpha2‐adrenergic autoinhibition.
ISSN:0077-8923
1749-6632
DOI:10.1196/annals.1304.033