Dopamine/serotonin receptor ligands. Part VIII[1]:the dopamine receptor antagonist LE300 - modelled and X-ray structure plus further pharmacological characterization, including serotonin receptor binding, biogenic amine transporter testing and in vivo testings

2004 ◽  
Vol 39 (6) ◽  
pp. 481-489 ◽  
Author(s):  
Michael Decker ◽  
Klaus-Jürgen Schleifer ◽  
Martin Nieger ◽  
Jochen Lehmann
Keyword(s):  
Receptor Antagonist ◽  
Receptor Binding ◽  
Biogenic Amine ◽  
Serotonin Receptor ◽  
Receptor Ligands ◽  
Pharmacological Characterization ◽  
Dopamine Receptor Antagonist ◽  
X Ray ◽  
Serotonin Receptor Binding

An approach for serotonin depletion in pigs: Effects on serotonin receptor binding

Synapse ◽  
2010 ◽  
Vol 65 (2) ◽  
pp. 136-145 ◽  
Author(s):  
Anders Ettrup ◽  
Birgitte R. Kornum ◽  
Pia Weikop ◽  
Gitte M. Knudsen
Keyword(s):  
Receptor Binding ◽  
Serotonin Receptor ◽  
Serotonin Depletion ◽  
Serotonin Receptor Binding

scholarly journals The dopamine receptor antagonist trifluoperazine prevents phenotype conversion and improves survival in mouse models of glioblastoma

2020 ◽  
Vol 117 (20) ◽  
pp. 11085-11096 ◽  
Author(s):  
Kruttika Bhat ◽  
Mohammad Saki ◽  
Erina Vlashi ◽  
Fei Cheng ◽  
Sara Duhachek-Muggy ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dopamine Receptor ◽  
Mouse Models ◽  
Radiation Sensitivity ◽  
Adult Brain ◽  
Continuous Treatment ◽  
Cell Phenotype ◽  
Dopamine Receptor Antagonist ◽  
Radiation Induced

Glioblastoma (GBM) is the deadliest adult brain cancer, and all patients ultimately succumb to the disease. Radiation therapy (RT) provides survival benefit of 6 mo over surgery alone, but these results have not improved in decades. We report that radiation induces a glioma-initiating cell phenotype, and we have identified trifluoperazine (TFP) as a compound that interferes with this phenotype conversion. TFP causes loss of radiation-induced Nanog mRNA expression, and activation of GSK3 with consecutive posttranslational reduction in p-Akt, Sox2, and β-catenin protein levels. TFP did not alter the intrinsic radiation sensitivity of glioma-initiating cells (GICs). Continuous treatment with TFP and a single dose of radiation reduced the number of GICs in vivo and prolonged survival in syngeneic and patient-derived orthotopic xenograft (PDOX) mouse models of GBM. Our findings suggest that the combination of a dopamine receptor antagonist with radiation enhances the efficacy of RT in GBM by preventing radiation-induced phenotype conversion of radiosensitive non-GICs into treatment-resistant, induced GICs (iGICs).

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