Abstract
The benzodiazepine receptor ligand iomazenil was labelled with carbon-11 to allow a direct positron emission tomography/single-photon emission tomography (PET/SPET) comparison with the well-known iodine-123 labelled compound. Imaging showed the same regional distribution for both modalities. Blood sample activity was corrected for metabolites by extraction with chloroform and high-performance liquid chromatographic analysis. Metabolism is very fast: 5min after application more than 85% of the plasma activity is present as hydrophilic metabolites. Kinetic methods were used to obtain regional estimates of transport rate constants and receptor concentrations. A three-compartment model was employed which gave transport rate constants for brain uptake (K1) and the distribution volume for the specifically receptor bound compartment (DVS). K1 varied from 0.32 to 0.50ml/min per gram for the cortical regions, cerebellum, thalamus and striatum for PET and SPET. Mean DVS-PET and DVS-SPET values were, respectively, 23+/-5 and 31+/-5ml/g for the occipital cortex, 11+/-3 and 15+/-2ml/g for the cerebellum, 7+/-2 and 11+/-3ml/g for the thalamus, 5+/-3 and 10+/-3ml/g for the striatum, and 3+/-2 and 3+/-1ml/g for the pons. These values correlate...Continue Reading
References
Apr 21, 1977·Nature·R F Squires, C Brastrup
Nov 25, 1977·Science·H Möhler, T Okada
Apr 1, 1992·Neurology·E W JohnsonJ P Seibyl
Nov 1, 1992·International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology·S S ZoghbiR T Malison
Jan 1, 1991·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·L BarreJ C Baron
Jul 1, 1991·Nuclear Medicine Communications·P A SchubigerE Moser
Nov 1, 1991·Annals of Neurology·K A FreyD E Kuhl
Jan 1, 1988·Resuscitation·E GellerY Nevo
Aug 9, 1988·European Journal of Pharmacology·P HantrayeM Mazière
Apr 9, 1981·Nature·W HunkelerW Haefely
Jan 1, 1994·European Archives of Psychiatry and Clinical Neuroscience·S SchlegelO Benkert
Jul 1, 1994·Journal of Pharmaceutical Sciences·M S GandelmanR B Innis
May 1, 1994·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·M LaruelleP B Hoffer
May 1, 1994·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·M LaruelleR B Innis
Jul 1, 1993·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J C PriceJ J Frost
Aug 1, 1993·Nuclear Medicine Communications·N P VerhoeffE A Van Royen
Citations
Dec 1, 1999·Synapse·J D BremnerR Baldwin
May 1, 1996·European Journal of Nuclear Medicine·C Burger, A Buck
Jul 1, 1996·European Journal of Nuclear Medicine·J T KuikkaL Farde
Nov 1, 1996·European Journal of Nuclear Medicine·Y OnishiT Mukai
Aug 31, 2013·Current Neurology and Neuroscience Reports·Henning Boecker
Oct 9, 1999·Psychiatry Research·J D BremnerR B Innis
May 22, 1998·Clinical Nuclear Medicine·J HashimotoY Fukuuchi
Apr 12, 2005·Nuclear Medicine and Biology·Young Soo ChangMyung Chul Lee
Nov 18, 2000·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·P MilletV Ibáñez
Jan 12, 2013·PloS One·Tihomir RuganiDavid Hladnik
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Jan D Andersson, Christer Halldin
Mar 1, 1997·European Journal of Nuclear Medicine·M H BourguignonB Mazière