Fluphenazine-N-2-chloroethane (hydrochloride) - CAS 3892-78-2

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 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.

CaMK, Others

Others, Neuroscience

3892-78-2

C22H27Cl3F3N3S

528.89

FC(F)(C1=CC=C2SC3=C(N(CCCN4CCN(CC4)CCCl)C2=C1)C=CC=C3)F.Cl.Cl

-20°C

Ice Packs

Small Compound