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T8516 Sigma

Trifluoperazine dihydrochloride

≥99%, powder

Synonym: 10-[3-(4-Methylpiperazin-1-yl)propyl]-2-(trifluoromethyl)-10H-phenothiazine dihydrochloride



Related Categories Application Index, Bioactive Small Molecule Alphabetical Index, Bioactive Small Molecules, Biochemicals and Reagents, Calcium Antagonists,
assay   ≥99%
form   powder
color   white to off-white
mp   243 °C (dec.)(lit.)
solubility   ethanol: soluble5 mg/mL
  H2O: soluble50 mg/mL, clear, colorless to yellow
  DMSO: soluble
storage temp.   −20°C
Gene Information   human ... DRD2(1813)



5, 10 g in glass bottle

Preparation Note

Trifluoperazine dihydrochloride dissolves in water at 50 mg/ml, with heat as required, and yields a clear, colorless to yellow solution. It is also soluble in DMSO and ethanol (5 mg/ml).


Trifluoperazine dihydrochloride has been used as a calmodulin kinase antagonist in cultured Aplysia californica neurons1. Trifluoperazine dihydrochloride has also been used as a PMCA inhibitor in mouse duodenal tissues to block the transcellular active calcium flux2.

Biochem/physiol Actions

Phenothiazine antipsychotic; D2 dopamine receptor antagonist; inhibits calmodulin-dependent stimulation of 3′:5′-cyclic nucleotide phosphodiesterase; inhibits cAMP-gated cation channels.

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®,1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.

This compound is featured on the Potassium Channels page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

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Safety Information

GHS07  GHS07
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Protocols & Articles
Peer-Reviewed Papers


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1. Activity-dependent initiation of a prolonged depolarization in aplysia bag cell neurons: role for a cation channel. Hung AY and Magoski NS J. Neurophysiol. 97(3), 2465-79, (2007)


2. Fibroblast growth factor-23 negates 1,25(OH)2D3-induced intestinal calcium transport by reducing the transcellular and paracellular calcium fluxes. Khuituan P, Wongdee K, Jantarajit W, et al. Arch. Biochem. Biophys. 536(1), 46-52, (2013)


The sarcolemmal Ca2+-ATPase of the ischemic-reperfused myocardium: protective effect of hypocalcemia on calmodulin-stimulated activity. Samouilidou, E.C., et al. Life Sci. 62, 29-36, (1998)


Characterization of calcineurin in human neutrophils Inhibitory effect of hydrogen peroxide on its enzyme activity and on NF-κB DNA binding. Carballo, M J. Biol. Chem. 274, 93, (1999)


Ca2+-calmodulin antagonists interfere with xylanase formation and secretion in Trichoderma reesei. Mach, R.L., et al. Biochim. Biophys. Acta 1403, 281-289, (1998)


Evaluation of the in vitro/in vivo potential of five berries (bilberry, blueberry, cranberry, elderberry, and raspberry ketones) commonly used as herbal supplements to inhibit uridine diphospho-glucuronosyltransferase. Choi EJ, Park JB, Yoon KD, et al. Food Chem. Toxicol. 72, 13-9, (2014)


Repurposing the antipsychotic trifluoperazine as an antimetastasis agent. Pulkoski-Gross A, Li J, Zheng C, et al. Mol. Pharmacol. 87(3), 501-12, (2015)


Combinatorial therapy with tamoxifen and trifluoperazine effectively inhibits malignant peripheral nerve sheath tumor growth by targeting complementary signaling cascades. Brosius SN, Turk AN, Byer SJ, et al. J. Neuropathol. Exp. Neurol. 73(11), 1078-90, (2014)


Metabolic drug-drug interaction potential of macrolactin A and 7-O-succinyl macrolactin A assessed by evaluating cytochrome P450 inhibition and induction and UDP-glucuronosyltransferase inhibition in vitro. Bae SH, Kwon MJ, Park JB, et al. Antimicrob. Agents Chemother. 58(9), 5036-46, (2014)


Evaluation of the in vitro/in vivo drug interaction potential of BST204, a purified dry extract of ginseng, and its four bioactive ginsenosides through cytochrome P450 inhibition/induction and UDP-glucuronosyltransferase inhibition. Zheng YF, Bae SH, Choi EJ, et al. Food Chem. Toxicol. 68, 117-27, (2014)


In vitro selective inhibition of human UDP-glucuronosyltransferase (UGT) 1A4 by finasteride, and prediction of in vivo drug-drug interactions. Lee SJ, Park JB, Kim D, et al. Toxicol. Lett. 232(2), 458-65, (2015)


Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum. Jing Yuan et al Nat. Chem. Biol. 5, 765-71, (2009)


Merck 14,9680

Beil. 27,IV,1353

Corp MSDS 1 (2), 3437:D / FT-IR 2 (2), 2236:A / FT-NMR 1 (2), 669:C / RegBook 1 (1), 1533:I / Sigma FT-IR 1 (2), 946:B / Structure Index 1, 239:C:5

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