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. 2019 Jul;370(1):111–126. doi: 10.1124/jpet.119.256818

TABLE 6.

D2 antagonist efficacy in animal studies

Compound Dose (mg/kg) Timing Model Efficacy Source Note
Bromocriptine 1 to 2 QD MNNG-induced Wistar rats (gastric cancer) ∼2.5-Fold increase in tumor number Iishi et al. (1992) Agonist
Chlorpromazine 10 QD×5 OVCAR-3 Xenograft, nude mice 64% Tumor growth suppression Choi et al. (2008)
Chlorpromazine 20 QD U87MG Xenograft 43.5% Inhibition of tumor growth Shin et al. (2013)
Fluphenazine 10 QD×5 OVCAR-3 Xenograft, nude mice Toxicity - ND Choi et al. (2008)
Haloperidol 10 QD MiaPaCa-2 Xenograft in NSG mice ∼50% Decrease in tumor mass Jandaghi et al. (2016)
Haloperidol 10 QD U87MG Xenograft No significant reductions in tumor size or survival Li et al. (2014) Synergy with AG1478
Imipramine 40 QD GRLp53het Mice 2-Fold increase in survival time over control Shchors et al. (2015) Cooperated with ticlopidine to enhance autophagy and increase survival
L-741,742 20 QD G362 Xenograft, flank and intracranial 40.9% Reduction in tumor mass, prolonged survival Dolma et al. (2016) Synergy with TMZ
Penfluridol 10 QD 4T1 Orthotopic mammary xenografts, female Balb/c mice 49% Reduction in tumor size Ranjan and Srivastava (2016)
Penfluridol 10 QD 4T1-luc Intracardiac metastasis model, female Balb/c 90% Reduction in brain fluorescence from luciferase reporter Ranjan and Srivastava (2016)
Penfluridol 10 QD 4T1 Intracranial xenograft ∼33% Reduction in brain fluorescence from luciferase reporter Ranjan and Srivastava (2016)
Penfluridol 10 QD BxPC-3 Xenografts (subcutaneous) in athymic nude mice ∼50% Reduction in tumor volume at day 27 Ranjan and Srivastava (2016)
Perphenazine 10 QD hTALL2 Cells in NSG mice ∼33% Reduction in luciferase bioluminescence Gutierrez et al. (2014)
Pnu 96415e 20 QD G362 Xenograft, flank 44.3% Reduction in tumor mass Dolma et al. (2016)
Quinpirole 10 QD LLC1 Xenograft ∼66% Reduction in bioluminescence Hoeppner et al. (2015) Agonist
Thioridazine 10 QD×5 OVCAR-3 Xenograft, nude mice 26% Tumor growth suppression Choi et al. (2008)
Thioridazine Pretreatment of cells NCI-N87 Xenograft Slight, insignificant reductions in tumor size or survival Mu et al. (2014) Pretreatment with 5 µm thioridazine
Thioridazine 300 μg/animal QD Ocl-Ly10 Xenograft, nude mice Nagel et al. (2012)
Thioridazine 25 QD 2774 Xenografts, nude mice >50% Reduction in tumor size and volume, significantly reduced Ki67 staining Park et al. (2014) Oral delivery
Thioridazine 32 QD 4T1 Xenograft in BALB/c 55% Reduction in tumor volume Yin et al. (2015)
Thioridazine Pretreatment of cells NCI-H1299 ∼50% Reduction in tumor size at day 47 Yue et al. (2016)
Trifluoperazine 10 2×/wk MDA-MB-231 Xenografts, nude mice ∼50% Reduction in tumor volume at day 33 Park et al. (2016)
Trifluoperazine 5 QD CL97 Tail vein injection NOD/SCID Significant reduction in bioluminescence/tumor size Yeh et al. (2012)
Trifluoperazine 10 QD×5 OVCAR-3 Xenograft, nude mice 46% Tumor growth suppression Choi et al. (2008)