Fluphenazine-N-2-chloroethane (hydrochloride) (Synonyms: Fluphenazine-N-mustard, FNM, FPCE, SKF-7171A) |
| カタログ番号GC43689 |
フルペナジンは、ドーパミンD2受容体に強く結合する従来の抗精神病薬化合物であり（Ki = 0.55 nM）、マイクロモル濃度でカルモジュリンを可逆的に阻害します。
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Cas No.: 3892-78-2
Sample solution is provided at 25 µL, 10mM.
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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.
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