The high-affinity peripheral benzodiazepine receptor ligand [C-11]DAA1106 results in improved delineation of neuroinflammatory lesions in a rodent model of disease compared to [C-11]PK11195

NeuroImage ◽  
2006 ◽  
Vol 31 ◽  
pp. T134 ◽  
Author(s):  
Brian Lopresti ◽  
S. Venneti ◽  
G. Wang ◽  
N.S. Mason ◽  
C.A. Mathis ◽  
...  
Keyword(s):  
Benzodiazepine Receptor ◽  
Rodent Model ◽  
Peripheral Benzodiazepine Receptor ◽  
Receptor Ligand ◽  
High Affinity

The peripheral benzodiazepine receptor ligand PK11195 overcomes different resistance mechanisms to sensitize AML cells to gemtuzumab ozogamicin

Blood ◽  
2004 ◽  
Vol 103 (11) ◽  
pp. 4276-4284 ◽  
Author(s):  
Roland B. Walter ◽  
Brian W. Raden ◽  
Michelle R. Cronk ◽  
Irwin D. Bernstein ◽  
Frederick R. Appelbaum ◽  
...  
Keyword(s):  
Drug Transport ◽  
Drug Transporters ◽  
Single Agent ◽  
Benzodiazepine Receptor ◽  
Resistance Mechanisms ◽  
Gemtuzumab Ozogamicin ◽  
Peripheral Benzodiazepine Receptor ◽  
Receptor Ligand ◽  
Antiapoptotic Proteins ◽  
Resistance Protein

Abstract The antibody-targeted therapeutic, gemtuzumab ozogamicin (GO, Mylotarg), is approved for treatment of relapsed acute myeloid leukemia (AML). We previously showed that AML blasts from GO refractory patients frequently express the drug transporters P-glycoprotein (Pgp) and/or multidrug resistance protein (MRP). We also previously reported that inhibition of drug transport by the Pgp modulator, cyclosporine A (CSA), can increase GO sensitivity in Pgp+ AML cells and that the peripheral benzodiazepine receptor ligand, PK11195, sensitizes AML cells to standard chemotherapeutics both by inhibiting Pgp-mediated efflux and by promoting mitochondrial apoptosis. We now show that PK11195 also can overcome multiple resistance mechanisms to increase GO sensitivity in AML cells, including resistance associated with expression of drug transporters and/or antiapoptotic proteins. PK11195 substantially increases GO cytotoxicity in AML cells from many different cell lines and primary patient samples, often more effectively than CSA. We also show that PK11195 is nontoxic in NOD/SCID mice and can sensitize xenografted human AML cells to GO. Since PK11195 is well tolerated in humans as a single agent, its further study as a multifunctional chemosensitizer for anti-AML therapies, including GO-based therapies, is warranted. (Blood. 2004;103:4276-4284)

Anxioselective properties of 6,3′-dinitroflavone, a high-affinity benzodiazepine receptor ligand

1996 ◽  
Vol 318 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Claudia Wolfman ◽  
Haydeé Viola ◽  
Mariel Marder ◽  
Cristina Wasowski ◽  
Patricia Ardenghi ◽  
...  
Keyword(s):  
Benzodiazepine Receptor ◽  
Receptor Ligand ◽  
High Affinity
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