Specific inhibition by burimamide of histamine effects on myocardial contraction and cyclic AMP
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In the isolated perfused guinea-pig heart, the increases in isotonic contraction and in cyclic AMP, produced by 2 μg of histamine were significantly and almost completely inhibited in the presence of 2 mg of burimamide, whereas the adrenergic β-receptor blocking drug Kö 592 (50 μg) was ineffective.
Under the same conditions similar effects of 0.1 μg of isoprenaline, which was equieffective with 2 μg of histamine, were not changed by 2 mg of burimamide, but prevented by 50 μg of Kö 592.
The results support the hypothesis, that histamine exerts its cardiac effects by stimulation of a receptor (H2) that can be clearly distinguished from the adrenergic (β1) receptor. The close parallelism between changes in contractile amplitude and in cyclic AMP produced by histamine in the absence and in the presence of burimamide is in accordance with the concept that cyclic AMP mediates the mechanical response of the heart to histamide.
Key wordsHeart-Contraction Cyclic AMP Histamine Burimamide
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