In vitro screen of inhibitors of rat brain serotonin synthesis

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Abstract
Over 700 compounds were screened at 10−4 M concentration as inhibitors of the conversion of L-tryptophan-14C to serotonin-14C in crude rat brain homogenates. Most of the compounds had little or no inhibitory effect. Those with strong inhibitory properties were tested as inhibitors of 5-hydroxytryptophan decarboxylase and, if active on the decarboxylase, were assayed as tryptophan hydroxylase inhibitors. Except for a few oxidizing and complexing agents and for some substituted p-phenylenediamines, the compounds found to inhibit tryptophan hydroxylase by >50% belonged to the three types of inhibitors already known, i.e. catechols, phenylalanine and ring-substituted phenylalanines, and 6-substituted tryptophans. The numerous data in this screen make possible some comments as to the structural requirements for activity within each class. A comparison of the results on tryptophan hydroxylase with data on tyrosine hydroxylase inhibition in similar homogenates makes it clear that two separate, if somewhat similar, enzymes are involved.

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