Effects of the imidazoline ligands efaroxan and KU14R on blood glucose homeostasis in the mouse

The putative imidazoline I 3 receptor antagonist 2-(2-ethyl-2,3-dihydrobenzo[ b]furan-2-yl)-1 H-imidazole (KU14R) has been shown to block the effects of the atypical I 3 agonist efaroxan at the level of the ATP-sensitive K + (K ATP) channel in isolated pancreatic islet β cells, but its effects in vi...

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Bibliographic Details
Published in:European journal of pharmacology 2002-11, Vol.454 (1), p.95-102
Main Authors: Mayer, Gaëll, Taberner, Peter V
Format: Article
Language:English
Subjects:
Adrenergic alpha-Agonists - pharmacology
Adrenergic alpha-Antagonists - pharmacology
Animals
Benzofurans - pharmacology
Blood glucose
Blood Glucose - metabolism
Brimonidine Tartrate
Dose-Response Relationship, Drug
Drug Interactions
Efaroxan
Electric Stimulation
Homeostasis
Hypoglycemic Agents - pharmacology
Imidazoles - pharmacology
Imidazoline
Imidazoline Receptors
In Vitro Techniques
Insulin
Insulin - blood
KU14R
Ligands
Male
Mice
Mice, Inbred CBA
Piperazines - pharmacology
Quinoxalines - pharmacology
Receptors, Drug - antagonists & inhibitors
Time Factors
Vas Deferens - drug effects
Vas Deferens - physiology
α 2-Adrenoceptor
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Description
Summary:The putative imidazoline I 3 receptor antagonist 2-(2-ethyl-2,3-dihydrobenzo[ b]furan-2-yl)-1 H-imidazole (KU14R) has been shown to block the effects of the atypical I 3 agonist efaroxan at the level of the ATP-sensitive K + (K ATP) channel in isolated pancreatic islet β cells, but its effects in vivo are not known. We have therefore investigated the effects of KU14R on blood glucose and insulin level in vivo. When KU14R was administered before or after a hypoglycaemic dose of efaroxan, the fall in blood glucose was at least additive. When the antihyperglycaemic imidazoline ligand S22068 was administered after a dose of KU14R, it did not alter the hypoglycaemic response. In the mouse isolated vas deferens preparation, neither rauwolscine (at concentrations which competitively antagonised the inhibitory response to 5-bromo-6-(2-imidazolin-2-ylamino)-quinoxaline (UK14304)) nor KU14R affected inhibition produced by S22068. At 10 −4 M, KU14R had weak α 2-adrenoceptor antagonist activity. We conclude that KU14R does not act as an antagonist of either efaroxan or S22068 at an imidazoline site in vivo.
ISSN:0014-2999
1879-0712
DOI:10.1016/S0014-2999(02)02473-1