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Journal of Pharmacology And Experimental Therapeutics, Vol. 153, Issue 1, 8-14, 1966
Copyright © 1966 by American Society for Pharmacology and Experimental Therapeutics

THE PHYSIOLOGIC DISPOSITION OF H3-HISTAMINE IN THE RAT BRAIN

Solomon H. Synder 1, Jacques Glowinski 1, and Julius Axelrod 1

1 Laboratory of Clinical Science, National Institute of Mental Health, National Institutes of Health, Bethesda, Maryland

The physiologic disposition of H3-histamine in rat brain has been studied after its intraventricular administration. H3-histamine is taken up and retained in the brain. H3-histamine disappears from the brain in a multiphasic fashion with a half-life of 1.6 hr during the first 6 hr and a half-life of 11 hr from 6 to 24 hr. The major metabolic product of H3-histamine in brain is H3 imidazoleacetic acid; a minor product is H3-methylhistamine. Subcellular distribution studies using a continuous sucrose gradient showed that the H3-histamine is highly localized in the pinched-off nerve ending and microsomal fractions. Monoamine oxidase inhibition elevates H3-histamine levels in rat brain. Reserpine and aminoguanidine have no effect.

Accepted on February 16, 1966




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Copyright © 1966 by the American Society for Pharmacology and Experimental Therapeutics.