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Stimulation of cerebral histamine H2 receptors by clonidine

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Abstract

CLONIDINE (2-[(2,6-dichlorophenyl)amino]-2-imidazoline) is a potent antihypertensive agent whose site of action is believed to be in the central nervous system1 but its mechanism of action is far from clear. Because of its effects on peripheral tissue, it has been generally accepted that the drug stimulates alpha-adrenergic receptors1. A recent report has, however, challenged this view: far from stimulating the receptors responsible for the accumulation of cyclic AMP in rat cortex, the drug seems to act as a potent alpha-adrenergic antagonist2. On the other hand, clonidine has been reported to stimulate gastric secretion by activation of histamine H2 receptors3. It was therefore of interest to check whether clonidine could also act on H2 receptors in brain tissues where they have been characterised4–6. We now report that clonidine strongly stimulates the accumulation of cyclic AMP in slices from guinea pig brain through activation of H2 receptors.

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Authors and Affiliations

  1. Unité 109 de Neurobiologie, 2ter rue d'Alésia, 75014, Paris, France

    YVES AUDIGIER, ALAIN VIRION & JEAN-CHARLES SCHWARTZ

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  1. YVES AUDIGIER
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  2. ALAIN VIRION
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  3. JEAN-CHARLES SCHWARTZ
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AUDIGIER, Y., VIRION, A. & SCHWARTZ, JC. Stimulation of cerebral histamine H2 receptors by clonidine. Nature 262, 307–308 (1976). https://doi.org/10.1038/262307a0

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