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Molecular Pharmacology

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Research ArticleArticle

Coupling of I1 Imidazoline Receptors to the cAMP Pathway: Studies with a Highly Selective Ligand, Benazoline

Hugues Greney, Philippe Ronde, Céline Magnier, Françoise Maranca, Carla Rascente, Wilma Quaglia, Mario Giannella, Maria Pigini, Livio Brasili, Claire Lugnier, Pascal Bousquet and Monique Dontenwill
Molecular Pharmacology June 2000, 57 (6) 1142-1151;
Hugues Greney
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Philippe Ronde
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Céline Magnier
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Françoise Maranca
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Carla Rascente
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Wilma Quaglia
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Mario Giannella
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Maria Pigini
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Livio Brasili
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Claire Lugnier
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Pascal Bousquet
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Monique Dontenwill
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Abstract

Clonidine and benazoline are two structurally related imidazolines. Whereas clonidine binds both to α2-adrenoceptors (α2R) and to I1 imidazoline receptors (I1R), benazoline showed a high selectivity for imidazoline receptors. Although the α2R are negatively coupled to adenylate cyclase, no effect on cAMP level by activation of I1R has been reported so far. We therefore aimed to compare the effects of clonidine and benazoline on forskolin-stimulated cAMP levels in cell lines expressing either I1R only (PC12 cells), α2R only (HT29 cells), or I1R and α2R together (NG10815 cells). Clonidine proved able to decrease the forskolin-stimulated cAMP level in the cells expressing α2R and this effect could be blocked by rauwolscine. In contrast, in cells lacking these adrenoceptors, clonidine had no effect. On the other hand, benazoline and other I1receptor-selective imidazolines decreased forskolin-stimulated cAMP level in the cells expressing I1R, in a rauwolscine- and pertussis toxin-insensitive manner. These effects were antagonized by clonidine. According to these results, we demonstrated that 1) α2R and I1R are definitely different entities because they are expressed independently in different cell lines; 2) α2R and I1R are both implicated in the cAMP pathway in cells (one is sensitive to pertussis toxin and the other is not); and 3) I1R might be coupled to more then one transduction pathway. These new data will be essential to further understand the physiological implications of the I1R and the functional interactions between I1 receptors and α2-adrenoceptors.

Footnotes

  • Send reprint requests to: Dr. M. Dontenwill, Lab. de Neurobiologie et Pharmacologie Cardiovasculaire, Faculté de Medecine, Univ. L. Pasteur, 11 rue Humann, 67000 Strasbourg, France. E-mail:monique.dontenwill{at}medecine.ustrasbg.fr

  • Abbreviations:
    DAG
    diacylglycerol
    PC
    phosphatidyl choline
    PL
    phospholipase
    PTX
    pertussis toxin
    DMEM
    Dulbecco's modified Eagle's medium
    FBS
    fetal bovine serum
    PIC
    paraiodoclonidine
    PDE
    phosphodiesterase
    PIPES
    1,4-piperazinediethanesulfonic acid
    CHAPS
    3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonic acid
    [Ca2+]i
    intracellular free calcium concentration
    • Received July 29, 1999.
    • Accepted February 9, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 57 (6)
Molecular Pharmacology
Vol. 57, Issue 6
1 Jun 2000
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Research ArticleArticle

Coupling of I1 Imidazoline Receptors to the cAMP Pathway: Studies with a Highly Selective Ligand, Benazoline

Hugues Greney, Philippe Ronde, Céline Magnier, Françoise Maranca, Carla Rascente, Wilma Quaglia, Mario Giannella, Maria Pigini, Livio Brasili, Claire Lugnier, Pascal Bousquet and Monique Dontenwill
Molecular Pharmacology June 1, 2000, 57 (6) 1142-1151;

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Research ArticleArticle

Coupling of I1 Imidazoline Receptors to the cAMP Pathway: Studies with a Highly Selective Ligand, Benazoline

Hugues Greney, Philippe Ronde, Céline Magnier, Françoise Maranca, Carla Rascente, Wilma Quaglia, Mario Giannella, Maria Pigini, Livio Brasili, Claire Lugnier, Pascal Bousquet and Monique Dontenwill
Molecular Pharmacology June 1, 2000, 57 (6) 1142-1151;
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