Hemodynamic effects and histamine release elicited by the selective adenosine A sub(3) receptor agonist 2-Cl-IB-MECA in conscious rats

The hemodynamic effects of the novel, selective adenosine A sub(3) receptor agonist 2-chloro-N super(6)-(3-iodobenzyl)adenosine 5'-N-methylcarboxamide (2-Cl-IB-MECA) were investigated in conscious rats. Intravenous administration of 200 mu g/kg 2-Cl-IB-MECA resulted in a short-lasting hypotensi...

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Bibliographic Details
Published in:European journal of pharmacology 1996-07, Vol.308 (3), p.311-314
Main Authors: Van Schaick, EA, Jacobson, KA, Kim, HO, Ijzerman, A P, Danhof, M
Format: Article
Language:English
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Summary:The hemodynamic effects of the novel, selective adenosine A sub(3) receptor agonist 2-chloro-N super(6)-(3-iodobenzyl)adenosine 5'-N-methylcarboxamide (2-Cl-IB-MECA) were investigated in conscious rats. Intravenous administration of 200 mu g/kg 2-Cl-IB-MECA resulted in a short-lasting hypotension, which was accompanied by a 50-100-fold increase in plasma histamine concentrations. Administration of a second dose of 2-Cl-IB-MECA did not elicit any hemodynamic effects. Also no histamine release was observed after the second dose. The observation of rapid tachyphylaxis in combination with histamine release suggests that mast cell mediator release plays a key role in the hemodynamic effects of adenosine A sub(3) receptor agonists.
ISSN:0014-2999