Thioridazine HCl

Thioridazine·HCl is a calcium channel protein inhibitor as well as D2DR/D4DR inhibitor. Its administration has been associated with hypotension. It has also been, after chronic treatment, used to test increased sensitivity of dopaminergic agents.

Flame atomic absorption determination of palladium in solutions after preconcentration using octadecyl silica membrane disks modified by thioridazine.HCl.[Pubmed:18969890]

Talanta. 2005 Feb 28;65(4):925-9.

A new simple and reliable method for rapid and selective extraction and determination of trace level of Pd(II) ion is developed. Palladium ions are adsorbed quantitatively during passage of aqueous samples through octadecyl silica membrane disks modified with thioridazine.HCl (TRH). The influence of flow rates of eluent and sample solution, amount of ligand, types and least amount of eluent, and pH of samples were studied. Almost all matrix elements were found to pass through the disk to drain. Break through volume and limit of detection of the membrane disks modified by 5mg of TRH was found to be 1.0 l and 12mugl(-1), respectively. The retained Pd(II) ions are then stripped from the disk with a minimal amount of sulfite solution as eluent and subsequently measured by atomic absorption spectrometry. The proposed method permitted large enrichment factors of about 100 and higher. The method was applied to the recovery of Pd(II) ions from different industrial samples and waters.

A comparison of the cardiovascular effects of haloperidol, thioridazine and chlorpromazine HCl.[Pubmed:6251766]

Arch Int Pharmacodyn Ther. 1980 Mar;244(1):48-57.

Transient hypotension, electrocardiographic conduction changes and cardiac arrhythmias have been reported with the use of certain anti-psychotic agents. To assess these observations, we compared the effects of haloperidol, thioridazine and chlorpromazine HCl on alpha-adrenergic receptors, mean aortic pressure, myocardial contractile force and myocardial electrophysiology in anesthetized dogs. The results from these studies indicated that, on a milligram basis, chlorpromazine HCl was equipotent to haloperidol, and thioridazine was 0.5 times as potent as haloperidol as an alpha-adrenergic receptor blocker and as a myocardial depressant. Each compound induced conduction nonhomogeneity in myocardial conducting tissue. However, as a neuroleptic, when tested in dogs, haloperidol was 50 times more potent than chlorpromazine HCl and 180 times more potent than thioridazine. The therapeutic safety indices (cardiovascular effect dose/neuroleptic dose) for haloperidol regarding alpha-adrenergic blockade, hypotension, myocardial depression and ventricular conduction delay were 4, 145, 235 and 125, respectively, whereas these indices for chlorpromazine and for thioridazine were 0.06, 2, 4, 6 and 0.05, 1, 3 and 1, respectively. Therefore, because of differences in neuroleptic potency, therapeutic doses of haloperidol are less likely to cause adverse cardiovascular effects than are those of either chlorpromazine HCl or thioridazine.

Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells.[Pubmed:22460505]

Apoptosis. 2012 Sep;17(9):989-97.

Recently, thioridazine (10-[2-(1-methyl-2-piperidyl) ethyl]-2-methylthiophenothiazine), a well-known anti-psychotic agent was found to have anti-cancer activity in cancer cells. However, the molecular mechanism of the agent in cellular signal pathways has not been well defined. Thioridazine significantly increased early- and late-stage apoptotic fraction in cervical and endometrial cancer cells, suggesting that suppression of cell growth by thioridazine was due to the induction of apoptosis. Cell cycle analysis indicated thioridazine induced the down-regulation of cyclin D1, cyclin A and CDK4, and the induction of p21 and p27, a cyclin-dependent kinase inhibitor. Additionally, we compared the influence of thioridazine with cisplatin used as a control, and similar patterns between the two drugs were observed in cervical and endometrial cancer cell lines. Furthermore, as expected, thioridazine successfully inhibited phosphorylation of Akt, phosphorylation of 4E-BP1 and phosphorylation of p70S6K, which is one of the best characterized targets of the mTOR complex cascade. These results suggest that thioridazine effectively suppresses tumor growth activity by targeting the PI3K/Akt/mTOR/p70S6K signaling pathway.

Identification of drugs including a dopamine receptor antagonist that selectively target cancer stem cells.[Pubmed:22632761]

Cell. 2012 Jun 8;149(6):1284-97.

Selective targeting of cancer stem cells (CSCs) offers promise for a new generation of therapeutics. However, assays for both human CSCs and normal stem cells that are amenable to robust biological screens are limited. Using a discovery platform that reveals differences between neoplastic and normal human pluripotent stem cells (hPSC), we identify small molecules from libraries of known compounds that induce differentiation to overcome neoplastic self-renewal. Surprisingly, thioridazine, an antipsychotic drug, selectively targets the neoplastic cells, and impairs human somatic CSCs capable of in vivo leukemic disease initiation while having no effect on normal blood SCs. The drug antagonizes dopamine receptors that are expressed on CSCs and on breast cancer cells as well. These results suggest that dopamine receptors may serve as a biomarker for diverse malignancies, demonstrate the utility of using neoplastic hPSCs for identifying CSC-targeting drugs, and provide support for the use of differentiation as a therapeutic strategy.

Selective inducer of CSC differentiation; anticancer agent,Thioridazine is an antipsychotic drug, used in the treatment of schizophrenia and psychosis, shows D4 selectivity or serotonin antagonism.

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