| Chemical Properties | Back Directory | [Melting point ]
224-225 °C | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 10 mg/ml; DMSO: 10 mg/ml; Ethanol: 1 mg/ml | [form ]
A crystalline solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
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]
| [storage]
Store at -20°C | [References]
[1] J D WINKLER B W K Thermos. Differential effects of fluphenazine-N-mustard, on calmodulin activity and on D1 and D2 dopaminergic responses.[J]. Psychopharmacology, 1987, 92 3: 285-291. DOI: 10.1007/bf00210832
[2] W N HAIT. Pharmacological properties of fluphenazine-mustard, an irreversible calmodulin antagonist.[J]. Molecular Pharmacology, 1987, 32 3: 404-409.
[3] Z H QIN. D2 dopamine receptor antisense oligodeoxynucleotide inhibits the synthesis of a functional pool of D2 dopamine receptors.[J]. Molecular Pharmacology, 1995, 48 4: 730-737.
[4] K. THERMOS B. W J D Winkler. Comparison of the effects of fluphenazine-n-mustard on dopamine binding sites and on behavior induced by apomorphine in supersensitive mice[J]. Neuropharmacology, 1987, 26 10: Pages 1473-1480. DOI: 10.1016/0028-3908(87)90166-3
[5] G DAVIDKOVA. D2 dopamine antisense RNA expression vector, unlike haloperidol, produces long-term inhibition of D2 dopamine-mediated behaviors without causing Up-regulation of D2 dopamine receptors.[J]. Journal of Pharmacology and Experimental Therapeutics, 1998, 285 3: 1187-1196.
[6] MI-KYUNG HWANG Seong H K Yong Ki Min. Calmodulin inhibition contributes to sensitize TRAIL-induced apoptosis in human lung cancer H1299 cells.[J]. Biochemistry and Cell Biology, 2009: 919-926. DOI: 10.1139/o09-058 |
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