3892-78-2 Basic information More..
Product Name:Fluphenazine-N-2-chloroethane (hydrochloride)
Synonyms:10-[3-[4-(2-chloroethyl)-1-piperazinyl]propyl]-2-(trifluoromethyl)-10H-phenothiazinedihydrochloride
CAS:3892-78-2
MF:C22H26Cl2F3N3S
MW:492.4281496
EINECS:
Mol File:3892-78-2.mol
3892-78-2

Use

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. Fluphenazine-N-2-chloroethane (hydrochloride) is a derivative of fluphenazine that contains an alkylating chlorethylamine chain, which produces irreversible protein binding. 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. Through this action, fluphenazine-B-2-chloroethane can be used to induce catalepsy in mice. It irreversibly inhibits calmodulin at higher doses (IC50 = 10 μM), which can sensitize cancer cells to TRAIL-induced apoptosis.[Cayman Chemical]

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