Literature DB >> 21365327

Human biodistribution and dosimetry of the PET radioligand [¹¹C]flumazenil (FMZ).

Charles M Laymon1, Rajesh Narendran, Neale S Mason, Jonathan P Carney, Brian J Lopresti, Chester A Mathis, James M Mountz, Donald Sashin, W Gordan Frankle.   

Abstract

PURPOSE: We measure the whole-body distribution of IV injected [¹¹C]Flumazenil (FMZ) as a function of time in adult subjects and determine the absorbed radiation doses. PROCEDURES: After injection with 770 MBq of [¹¹C]FMZ (nominal), each of six subjects underwent nine consecutive whole body PET scans. Twelve source organs were identified using PET attenuation and emission images. Activity within each organ as a function of time was determined from the sequence of the nine PET scans. Source organ time activity curves were integrated and normalized by the injected dose to yield source organ residence times for the no voiding situation. Separate bladder residence-time calculations were performed for the cases of a 1- and a 2-h voiding interval. Using the source organ residence times as input, the program OLINDA/EXM (Stabin et al. in J Nucl Med. 46:1023-1027, 2005) was used to perform dosimetry calculations for the various body organs and for the whole body.
RESULTS: For the no voiding situation, the average whole-body radiation equivalent dose was 3.02 × 10⁻³ mSv/MBq of injected [¹¹C]FMZ. The average effective dose and effective dose equivalent was 7.57 × 10⁻³ and 1.12 × 10⁻² mSv MBq⁻¹, respectively. The organ receiving the highest equivalent dose was the urinary bladder wall with an average of 6.32 × 10⁻² mSv MBq⁻¹.
CONCLUSION: On average, the administration of less than 790 MBq (21 mCi) of [¹¹C]FMZ yields (no voiding model) an organ equivalent dose of under 50 mSv [the single dose limit for research studies under US regulations (21CFR361.1) to body organs other than blood forming organs, gonads or the lens of the eye] to all organs. Equivalent dose to the blood forming organs and gonads from a 790 MBq administered FMZ dose is well under the 30 mSv limit provided under 21CFR361.1. Additionally, administration of less than 1320 MBq (35.7 mCi) yields an effective dose [International Commission on Radiation Protection (ICRP) 60 tissue weighting scheme] of under 10 mSv, which is the ICRP IIb (minor to intermediate) risk category limit.

Entities:  

Mesh:

Substances:

Year:  2012        PMID: 21365327     DOI: 10.1007/s11307-011-0478-2

Source DB:  PubMed          Journal:  Mol Imaging Biol        ISSN: 1536-1632            Impact factor:   3.488


  51 in total

1.  The 2007 Recommendations of the International Commission on Radiological Protection. ICRP publication 103.

Authors: 
Journal:  Ann ICRP       Date:  2007

2.  Impaired benzodiazepine receptor binding in peri-lesional cortex of patients with symptomatic epilepsies studied by [(11)C]-flumazenil PET.

Authors:  Brigitte Szelies; J Sobesky; G Pawlik; R Mielke; B Bauer; K Herholz; W-D Heiss
Journal:  Eur J Neurol       Date:  2002-03       Impact factor: 6.089

3.  Decreased GABA-A binding on FMZ-PET in succinic semialdehyde dehydrogenase deficiency.

Authors:  P L Pearl; K M Gibson; Z Quezado; I Dustin; J Taylor; S Trzcinski; J Schreiber; K Forester; P Reeves-Tyer; C Liew; S Shamim; P Herscovitch; R Carson; J Butman; C Jakobs; W Theodore
Journal:  Neurology       Date:  2009-08-11       Impact factor: 9.910

4.  Biodistribution and radiation dosimetry of the dopamine D2 ligand 11C-raclopride determined from human whole-body PET.

Authors:  Mark Slifstein; Dah-Ren Hwang; Diana Martinez; Jesper Ekelund; Yiyun Huang; Elizabeth Hackett; Anissa Abi-Dargham; Marc Laruelle
Journal:  J Nucl Med       Date:  2006-02       Impact factor: 10.057

5.  Tiagabine increases [11C]flumazenil binding in cortical brain regions in healthy control subjects.

Authors:  W Gordon Frankle; Raymond Y Cho; Rajesh Narendran; N Scott Mason; Shivangi Vora; Maralee Litschge; Julie C Price; David A Lewis; Chester A Mathis
Journal:  Neuropsychopharmacology       Date:  2008-07-09       Impact factor: 7.853

6.  Measurement of GABAA receptor binding in vivo with [11C]flumazenil: a test-retest study in healthy subjects.

Authors:  Elina Salmi; Sargo Aalto; Jussi Hirvonen; Jaakko W Långsjö; Anu T Maksimow; Vesa Oikonen; Liisa Metsähonkala; Jussi Virkkala; Kjell Någren; Harry Scheinin
Journal:  Neuroimage       Date:  2008-03-04       Impact factor: 6.556

7.  In vivo cerebral metabolism and central benzodiazepine-receptor binding in temporal lobe epilepsy.

Authors:  T R Henry; K A Frey; J C Sackellares; S Gilman; R A Koeppe; J A Brunberg; D A Ross; S Berent; A B Young; D E Kuhl
Journal:  Neurology       Date:  1993-10       Impact factor: 9.910

8.  Focal decreases of cortical GABAA receptor binding remote from the primary seizure focus: what do they indicate?

Authors:  Csaba Juhász; Eishi Asano; Aashit Shah; Diane C Chugani; Carlos E A Batista; Otto Muzik; Sandeep Sood; Harry T Chugani
Journal:  Epilepsia       Date:  2008-07-14       Impact factor: 5.864

9.  Regional specific binding of [11C]RO 15 1788 to central type benzodiazepine receptors in human brain: quantitative evaluation by PET.

Authors:  S Pappata; Y Samson; C Chavoix; C Prenant; M Mazière; J C Baron
Journal:  J Cereb Blood Flow Metab       Date:  1988-06       Impact factor: 6.200

10.  Quantification of benzodiazepine receptors in human brain using PET, [11C]flumazenil, and a single-experiment protocol.

Authors:  J Delforge; S Pappata; P Millet; Y Samson; B Bendriem; A Jobert; C Crouzel; A Syrota
Journal:  J Cereb Blood Flow Metab       Date:  1995-03       Impact factor: 6.200

View more
  4 in total

1.  Radiation dosimetry and biodistribution of the TSPO ligand 11C-DPA-713 in humans.

Authors:  Christopher J Endres; Jennifer M Coughlin; Kenneth L Gage; Crystal C Watkins; Michael Kassiou; Martin G Pomper
Journal:  J Nucl Med       Date:  2012-01-12       Impact factor: 10.057

2.  Biodistribution and Radiation Dosimetry for the Novel SV2A Radiotracer [(18)F]UCB-H: First-in-Human Study.

Authors:  F Bretin; M A Bahri; C Bernard; G Warnock; J Aerts; N Mestdagh; T Buchanan; C Otoul; F Koestler; F Mievis; F Giacomelli; C Degueldre; R Hustinx; A Luxen; A Seret; A Plenevaux; E Salmon
Journal:  Mol Imaging Biol       Date:  2015-08       Impact factor: 3.488

3.  11C Dosimetry Scans Should Be Abandoned.

Authors:  Paolo Zanotti-Fregonara; Adriaan A Lammertsma; Robert B Innis
Journal:  J Nucl Med       Date:  2020-12-11       Impact factor: 11.082

4.  Use of 55 PET radiotracers under approval of a Radioactive Drug Research Committee (RDRC).

Authors:  Isaac M Jackson; So Jeong Lee; Alexandra R Sowa; Melissa E Rodnick; Laura Bruton; Mara Clark; Sean Preshlock; Jill Rothley; Virginia E Rogers; Leslie E Botti; Bradford D Henderson; Brian G Hockley; Jovany Torres; David M Raffel; Allen F Brooks; Kirk A Frey; Michael R Kilbourn; Robert A Koeppe; Xia Shao; Peter J H Scott
Journal:  EJNMMI Radiopharm Chem       Date:  2020-11-11
  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.