PaperReverse transcriptase-polymerase chain reaction (RT-PCR) analysis of monoamine transporters in neuroblastoma cell lines: Correlations to meta-iodobenzylguanidine (MIBG) uptake and tyrosine hydroxylase gene expression
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2013, Neuroscience LettersCitation Excerpt :However the mechanisms underlying METH-induced cell death remain unclear. In the present study, dopaminergic SH-SY5Y cell lines were employed to test METH-induced toxicity in dopaminergic cells because they express TH [12] and have the capacity to uptake catecholamine [2]. Several lines of evidence have described the neurotoxicity of METH, for instance, the persistent depletion of dopaminergic neurons resulting from the mitochondria dysfunction [25] and ROS generation [5].
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2013, Brain Research BulletinSynthesis and serotonin transporter activity of 1,3-bis(aryl)-2-nitro-1- propenes as a new class of anticancer agents
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :The aziridine derivative was formed in high yields (62%) compared to the desired propanamine 5b (27%). A number of novel pyridines, dihydropyridone and N,N-di(1-aryl-2-propyl) amines described as route-specific byproducts associated with clandestine synthesis of 4-MTA and related amphetamines12 were previously evaluated for SERT-selective cytotoxicity using human embryonic kidney cells overexpressing SERT, and two malignant cell lines; the DG-75 cell line, which has been previously shown by our laboratory to express SERT2,13 and to the SHSY-5Y neuroblastoma cell line, which does not express SERT.23 As previously described, the compound of most interest from this study was the N-formyl-1,3-bis(4-methylthiophenyl)-2-propanamine (7a) (Fig. 1) which was found to be cytotoxic to the hSERT-overexpressing cell line and not to the HEK293 cell line implying a selective-SERT cytotoxic effect.12
Synthesis and serotonin transporter activity of sulphur-substituted α-alkyl phenethylamines as a new class of anticancer agents
2009, European Journal of Medicinal ChemistryCitation Excerpt :The DG-75 cell line is a B-lymphocyte, chemoresistant Burkitt's lymphoma cell line derived from a metastatic pleural effusion (lung) of a sporadic case of EBV (Epstein Barr Virus) negative Burkitt's lymphoma [62] that has been shown to express SERT (Supplemental Fig. 1). The SHSY-5Y cell line is a neuroblastoma cell line established from a metastatic bone tumour [63] that was chosen to use in the screen as it has been shown not to express SERT [64]. In this study using the Neutral Red assay it was found that a number of 4-MTA derivatives in particular the Type IIa derivatives showed potent cytotoxic activity toward the chemoresistant SERT expressing BL cell line DG-75 (Tables 1–5) and to the SHSY-5Y cell line with approximate pEC50 values of 5 correlating to an EC50 range of between 1 μM and 5 μM.