Fluphenazine-<wbr/>N-2-<wbr/>chloroethane (hydro<wbr>chloride)

Fluphenazine-N-2-chloroethane (hydrochloride)

CAT N°: 18427
Price:

48.00 40.80

Fluphenazine is a traditional antipsychotic compound that tightly binds the dopamine D2 receptor (Ki = 0.55 nM) and also reversibly inhibits calmodulin at micromolar concentrations.{26444,30053} Fluphenazine-N-2-chloroethane is a derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding.{30056,30051} It is a relatively selective, irreversible antagonist of D2 receptors both in vitro (IC50 = 100 nM) and in vivo, inactivating approximately 90% of D2 receptors in mice within 4 hours of treatment.{30054,30055} Through this action, fluphenazine-B-2-chloroethane can be used to induce catalepsy in mice.{30054,30050} It irreversibly inhibits calmodulin at higher doses (IC50 = 10 µM), which can sensitize cancer cells to TRAIL-induced apoptosis.{30056,30052}

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