Fluphenazine-N-2-chloroethane·2HCl (CAS 83016-35-7)
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Fluphenazine-N-2-chloroethane is a nitrogen mustard-containing derivative of Fluphenazine dihydrochloride (sc-211531) that demonstrates irreversible inhibition of CaM-induced activation of CNPase (cyclic nucleotide phosphodiesterase). Inclusion of the alkylating nitrogen mustard moiety in Fluphenazine-N-2-chloroethane produces irreversible deactivation of CaM, while the parent compound demonstrates a reversible inhibitory activity. CaM antagonism is shown to sensitize malignant cells to TRAIL (tumor necrosis factor related apoptosis-inducing ligand) necrotic signaling, promoting cell death in TRAIL-resistant growth. Fluphenazine-N-2-chloroethane is further shown to irreversibly antagonize dopamine receptors with selectivity for D2DR over D1DR. Inhibition of the dopamine receptors by Fluphenazine-N-2-chloroethane correlated to an increase in D2DR mRNA, a decrease in D1DR mRNA, and an increase in glutamic acid decarboxylase mRNA, indicating that this inhibition of dopamine receptor activity has a regulatory role in the cellular expression of dopaminergic and GABAergic proteins.
Fluphenazine-N-2-chloroethane·2HCl (CAS 83016-35-7) References
- Calmodulin inhibition contributes to sensitize TRAIL-induced apoptosis in human lung cancer H1299 cells. | Hwang, MK., et al. 2009. Biochem Cell Biol. 87: 919-26. PMID: 19935877
- Differential effects of fluphenazine-N-mustard, on calmodulin activity and on D1 and D2 dopaminergic responses. | Winkler, JD., et al. 1987. Psychopharmacology (Berl). 92: 285-91. PMID: 2957717
- Dual action of ketamine confines addiction liability. | Simmler, LD., et al. 2022. Nature. 608: 368-373. PMID: 35896744
- Pharmacological properties of fluphenazine-mustard, an irreversible calmodulin antagonist. | Hait, WN., et al. 1987. Mol Pharmacol. 32: 404-9. PMID: 3670276
- D2 dopamine receptor antisense oligodeoxynucleotide inhibits the synthesis of a functional pool of D2 dopamine receptors. | Qin, ZH., et al. 1995. Mol Pharmacol. 48: 730-7. PMID: 7476901
- Irreversible blockade of D2 dopamine receptors by fluphenazine-N-mustard increases D2 dopamine receptor mRNA and proenkephalin mRNA and decreases D1 dopamine receptor mRNA and mu and delta opioid receptors in rat striatum. | Chen, JF., et al. 1994. Neurochem Int. 25: 355-66. PMID: 7820070
- Irreversible blockade of D2 dopamine receptors by fluphenazine-N-mustard increases glutamic acid decarboxylase mRNA in rat striatum. | Chen, JF. and Weiss, B. 1993. Neurosci Lett. 150: 215-8. PMID: 8097031
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Fluphenazine-N-2-chloroethane·2HCl, 50 mg | sc-201502 | 50 mg | $67.00 |