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  • Title: Pentobarbitone inhibition of catecholamine secretion.
    Author: Holmes JC, Schneider FH.
    Journal: Br J Pharmacol; 1973 Oct; 49(2):205-13. PubMed ID: 4793439.
    Abstract:
    1. The perfused isolated cow adrenal gland was used to investigate the effect of barbituric acid, phenobarbitone and pentobarbitone on catecholamine secretion.2. Pentobarbitone reduced catecholamine secretion induced by a number of drugs which cause exocytosis. The concentration of pentobarbitone which caused a 50% inhibition of catecholamine secretion was for acetylcholine 5.6 x 10(-5)M, for carbachol 6.3 x 10(-5)M, for histamine 1.6 x 10(-4)M, for (+)-amphetamine 4.4 x 10(-5)M and for potassium chloride 1.5 x 10(-4)M. The degree of inhibition by pentobarbitone was not dependent on the concentration of the secretagogue.3. Pentobarbitone (up to 10(-3)M) did not inhibit the catecholamine release that was induced by acetyldehyde or by calcium chloride; it inhibited slightly (34%) the catecholamine secretion induced by tyramine.4. Catecholamine release induced by carbachol was also inhibited by phenobarbitone (50% inhibition at 2.8 x 10(-4)M (n=7)) but was unaffected by barbituric acid.5. Pentobarbitone had no effect on spontaneous or on (+)-amphetamine- or tyramine-induced release of catecholamines from isolated chromaffin vesicles of cow adrenal medulla.6. It is concluded that pentobarbitone inhibits catecholamine release by preventing a configurational change in the structure of the membrane of the chromaffin cell which is a necessary link between receptor activation and catecholamine release.
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