Hydrolytic biotransformation of the bumetanide ester prodrug DIMAEB to bumetanide by esterases in neonatal human and rat serum and neonatal rat brain—A new treatment strategy for neonatal seizures?

Objectives The loop diuretic bumetanide has been proposed previously as an adjunct treatment for neonatal seizures because bumetanide is thought to potentiate the action of γ‐aminobutyric acid (GABA)ergic drugs such as phenobarbital by preventing abnormal intracellular accumulation of chloride and t...

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Veröffentlicht in:	Epilepsia (Copenhagen) 2021-01, Vol.62 (1), p.269-278
Hauptverfasser:	Theilmann, Wiebke, Brandt, Claudia, Bohnhorst, Bettina, Winstroth, Anne‐Mieke, Das, Anibh Martin, Gramer, Martina, Kipper, Andi, Kalesse, Markus, Löscher, Wolfgang
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Animals, Newborn Biotransformation blood‐brain barrier Brain - enzymology Brain - metabolism BUM5 Bumetanide Bumetanide - metabolism carboxylesterase Convulsions & seizures Diuretics Drug therapy Esterase Esterases Esters - metabolism Female Humans Infant, Newborn Infants Lipophilic Male Neonates NKCC1 ontogenesis Phenobarbital Prodrugs Prodrugs - metabolism Rats Rodents Seizures Serum - enzymology Serum - metabolism γ-Aminobutyric acid
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