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Halopemide Phospholipase

Satisfactory Essays

IC50: 220 and 310 nM for human PLD1 and PLD2, respectively

Halopemide is a phospholipase D (PLD) inhibitor.

Phospholipase D (PLD) is a key enzyme for the production of phosphatidic acid, a lipid second messenger. Phosphatidic acid involves in both G protein-coupled receptor and receptor tyrosine kinase signal transduction networks.

In vitro: In a previous study, the IC50 of halopemide against PLD2 was found to be similar to that previously reported, but the compound had no preference for PLD2 over PLD1 [1].

In vivo: Animal study showed that the halopemide concentration in the rat brain was 10 times less than that of R29800, its chemical analog. However, the levels were the same in the pituitary gland. The highest level of halopemide was

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