Inhibition of histidine decarboxylase and diamine oxidase by 4-bromo-3-hydroxybenzyloxyamine

Autor: Kobayashi Yutaka, Jacob Kupelian, David V. Maudsley
Rok vydání: 1970
Předmět:
Zdroj: Biochemical Pharmacology. 19:1761-1770
ISSN: 0006-2952
DOI: 10.1016/0006-2952(70)90168-1
Popis: In freely fed rats, an intraperitoneal injection of 0.688 m-mole per kg of 4-bromo-3-hydroxybenzyloxyamine (NSD 1055) produces a transient drop in both the histidine decarboxylase activity of the glandular stomach and the diamine oxidase activity of the intestine. Both enzymes are inhibited by approximately 50 per cent within 30 min, but recovery to normal levels occurs within a few hours. The results obtained in vivo are in sharp contrast to the data in vitro , which show that the inhibitor is much more active against the decarboxylase. The transient effect of NSD 1055 against the two enzymes in vivo may be due primarily to the rapid clearance or metabolism of the drug, while the change in potency ratio from a situation in vitro to one in vivo may reflect the greater rate of turnover of histidine decarboxylase. The drug, however, is very effective in preventing the rise in histidine decarboxylase produced by insulin, pentagastrin or refeeding of starved animals. Presumably under these circumstances there is a greater opportunity for the drug to complex with the cofactor, pyridoxal phosphate.
Databáze: OpenAIRE