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Nordimaprit is a histamine H2 receptor agonist that has demonstrated the ability to decrease tyrosinase activity in cultured human melanoma cells. This leads to a significant reduction and eventual loss of pigment. Its mechanism of action involves three components: the induction of an inhibitory activity against tyrosinase, an increased rate of tyrosinase degradation, and a long-term down-regulation of tyrosinase expression. The depigmenting effect was shown to be long-lasting, with cells remaining amelanotic for weeks after drug removal.
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