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Title: Radio-methyl vorozole and methods for making and using the same

Patent ·
OSTI ID:1150092
; ;

Radiotracer vorozole compounds for in vivo and in vitro assaying, studying and imaging cytochrome P450 aromatase enzymes in humans, animals, and tissues and methods for making and using the same are provided. [N-radio-methyl] vorozole substantially separated from an N-3 radio-methyl isomer of vorozole is provided. Separation is accomplished through use of chromatography resins providing multiple mechanisms of selectivity.

Research Organization:
Brookhaven National Laboratory (BNL), Upton, NY (United States)
Sponsoring Organization:
USDOE
DOE Contract Number:
AC02-98CH10886
Assignee:
Brookhaven Science Associates, LLC (Upton, NY)
Patent Number(s):
8,802,053
Application Number:
13/847,136
OSTI ID:
1150092
Country of Publication:
United States
Language:
English

References (23)

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Reinvestigation of the synthesis and evaluation of [N-methyl-11C]vorozole, a radiotracer targeting cytochrome P450 aromatase journal April 2009
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Potential of Immobilized Artificial Membranes for Predicting Drug Penetration Across the Blood−Brain Barrier journal January 1998
Process for preparing enantiomerically pure 6-[(4-chlorophenyl) (1H-1,2,4-triazol-1-yl) methyl]-1-methyl-1H-benzotrizole patent September 1997
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Unique distribution of aromatase in the human brain: In vivo studies with PET and [N-methyl-11C]vorozole journal April 2010
Comparative evaluation of positron emission tomography radiotracers for imaging the norepinephrine transporter: (S,S) and (R,R) enantiomers of reboxetine analogs ([11C]methylreboxetine, 3-Cl-[11C]methylreboxetine and [18F]fluororeboxetine), (R)-[11C]nisox: Norepinephrine transporter radiotracers for PET journal June 2005
18F-Labelled vorozole analogues as PET tracer for aromatase journal January 2008
R 76713, a new specific non-steroidal aromatase inhibitor journal June 1989
Distribution of Aromatase Cytochrome P450 Messenger Ribonucleic Acid in Adult Rhesus Monkey Brains1 journal October 1997
Synthesis and PET studies of [11C-cyano]letrozole (Femara), an aromatase inhibitor drug journal February 2009
Comparative effects of the aromatase inhibitor R76713 and of its enantiomers R83839 and R83842 on steroid biosynthesis in vitro and in vivo journal December 1990
Chromatographic classification and comparison of commercially available reversed-phase liquid chromatographic columns containing phenyl moieties using principal component analysis journal June 2007
New non-steroidal aromatase inhibitors: Focus on R76713 journal November 1990
Development Summary towards a Manufacturable Process for R 83842 [( S )-6-[(4-chlorophenyl) (1H-1,2,4-triazol-1-yl)methyl]-1-methyl-1H-benzotriazole] † journal May 2000
Synthesis and activity of 1H-benzimidazole and 1H-benzotriazole derivatives as inhibitors of Acanthamoeba castellanii journal May 2004

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37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY