scholarly journals l‐Stepholidine is a potent pan‐dopamine receptor antagonist at G protein and β‐arrestin mediated signaling in vitro (662.5)

2014 ◽  
Vol 28 (S1) ◽  
Author(s):  
Julie Meade ◽  
R Free ◽  
Nicole Miller ◽  
Amy Moritz ◽  
Jennie Conroy ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dopamine Receptor ◽  
G Protein ◽  
Dopamine Receptor Antagonist

scholarly journals Combined Treatment with Dopamine Receptor Antagonists and Radiation Creates a Metabolic Vulnerability in Mouse Models of Glioblastoma

2020 ◽  
Author(s):  
Mohammad Saki ◽  
Kruttika Bhat ◽  
Fei Cheng ◽  
Ling He ◽  
Le Zhang ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dopamine Receptor ◽  
Mouse Models ◽  
Cholesterol Biosynthesis ◽  
Combined Treatment ◽  
Unmet Need ◽  
Survival Times ◽  
Self Renewal ◽  
Dopamine Receptor Antagonist

AbstractBackgroundGlioblastoma is the deadliest brain tumor in adults and the standard-of-care consists of surgery followed by radiation and treatment with temozolomide. Overall survival times for patients suffering from glioblastoma are unacceptably low indicating an unmet need for novel treatment options.MethodsUsing patient-derived glioblastoma lines and mouse models of glioblastoma we test the effect of radiation and the dopamine receptor antagonist on glioblastoma self-renewal in vitro and survival in vivo. A possible resistance mechanism is investigated using RNA-Sequencing.ResultsTreatment of glioma cells with the dopamine receptor antagonist quetiapine reduced glioma cell self-renewal in vitro and combined treatment of mice with quetiapine and radiation prolonged the survival of glioma-bearing animals. The combined treatment induced the expression of genes involved in cholesterol biosynthesis. This rendered the tumors vulnerable to simultaneous treatment with atorvastatin and further significantly prolonged the survival of the animals.ConclusionsOur results indicate high efficacy of a triple combination of quetiapine, atorvastatin and radiation against glioblastoma without increasing the toxicity of radiation. With both drugs readily available for clinical use our study could be rapidly translated into a clinical trial.

scholarly journals (-)-Stepholidine is a potent pan-dopamine receptor antagonist of both G protein- and β-arrestin-mediated signaling

2014 ◽  
Vol 232 (5) ◽  
pp. 917-930 ◽  
Author(s):  
Julie A. Meade ◽  
R. Benjamin Free ◽  
Nicole R. Miller ◽  
Lani S. Chun ◽  
Trevor B. Doyle ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dopamine Receptor ◽  
G Protein ◽  
Dopamine Receptor Antagonist

Spectrofluorimetric determination of dopamine receptor antagonist LE 300 in mice plasma

Luminescence ◽  
2015 ◽  
Vol 31 (1) ◽  
pp. 63-66 ◽  
Author(s):  
Mohamed Hefnawy ◽  
Mostafa Mohamed ◽  
Mohamed Abunassif ◽  
Amer Alanazi ◽  
Abdulrahman Al-Majed ◽  
...  
Keyword(s):  
Receptor Antagonist ◽  
Dopamine Receptor ◽  
Dopamine Receptor Antagonist ◽  
Spectrofluorimetric Determination
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