[(123)I]AM281 single-photon emission computed tomography imaging of central cannabinoid CB(1) receptors before and after Delta(9)-tetrahydrocannabinol therapy and whole-body scanning for assessment of radiation dose in tourette patients.

[(123)I]AM281 single-photon emission computed tomography imaging of central cannabinoid CB(1) receptors before and after Delta(9)-tetrahydrocannabinol therapy and whole-body scanning for assessment of radiation dose in tourette patients. Research Abstract Details 

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[(123)I]AM281 single-photon emission computed tomography imaging of central cannabinoid CB(1) receptors before and after Delta(9)-tetrahydrocannabinol therapy and whole-body scanning for assessment of radiation dose in tourette patients. Abstract Text:

Georg Berding,Kirsten ,Udo Schneider,Peter Gielow, Fitschen,Manfred Stuhrmann,Heinrich Harke,Ralph Buchert,Frank Donnerstag,Michael Hofmann,Bernd O Knoop,David J Brooks,Hinderk M Emrich,Wolfram H Knapp,Georg Berding,Kirsten ,Udo Schneider,Peter Gielow, Fitschen,Manfred Stuhrmann,Heinrich Harke,Ralph Buchert,Frank Donnerstag,Michael Hofmann,Bernd O Knoop,David J Brooks,Hinderk M Emrich,Wolfram H Knapp,Georg Berding,Kirsten ,Udo Schneider,Peter Gielow, Fitschen,Manfred Stuhrmann,Heinrich Harke,Ralph Buchert,Frank Donnerstag,Michael Hofmann,Bernd O Knoop,David J Brooks,Hinderk M Emrich,Wolfram H Knapp,

BACKGROUND: The cannabinoid CB(1) receptor agonist Delta(9)-THC has been suggested for treatment of Tourette syndrome (TS). Based on animal studies, the CB(1) antagonist [(123)I]AM281 (N-(Morpholin-4-yl)-1-(2,4-dichlorophenyl)-5-(4-[(123)I]iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide) has been proposed for single photon emission computed tomography (SPECT) in humans. Our aims were to 1) evaluate specific binding of [(123)I]AM281 to CB(1) receptors in TS patients and 2) assess radiation exposure associated with the use of AM281 labeled with (123)I for SPECT and (124)I for positron emission tomography. METHODS: We employed [(123)I]AM281 in six TS patients before and after Delta(9)-THC treatment. Dynamic SPECT, plasma measurements (including metabolite analysis with thin layer chromatography), and whole-body imaging were performed. Regions of interest derived from magnetic resonance images were used to extract from SPECT uptake in an area with high CB(1) density (lentiform nuclei) and reference regions. Specific over nonspecific partition coefficients V(3)" were calculated. Whole-body images were carried out for dosimetric analysis. Data obtained with [(123)I]AM281 were used to predict doses from [(124)I]AM281. RESULTS: Mean V(3)" ranged from.19 to.31 and did not change significantly after Delta(9)-THC treatment. Nevertheless, in the only patient with a marked clinical response, V(3)" clearly declined. Thin layer chromatography revealed biexponential kinetics of tracer metabolism; about 60% remained nonmetabolized after 3 hours. Effective doses of.011 mSv/MBq for [(123)I]AM281 and.34 for [(124)I]AM281 were computed. CONCLUSIONS: This study suggests that specific binding of [(123)I]AM281 to CB(1) receptors can be detected in patients using SPECT. Radiation exposure with [(123)I]AM281 is low; that with [(124)I]AM281 is higher but acceptable for single investigations.

[(123)I]AM281 single-photon emission computed tomography imaging of central cannabinoid CB(1) receptors before and after Delta(9)-tetrahydrocannabinol therapy and whole-body scanning for assessment of radiation dose in tourette patients. Publishing Authors By Initials

G Berding,K ,U Schneider,P Gielow,J Fitschen,M Stuhrmann,H Harke,R Buchert,F Donnerstag,M Hofmann,BO Knoop,DJ Brooks,HM Emrich,WH Knapp,G Berding,K ,U Schneider,P Gielow,J Fitschen,M Stuhrmann,H Harke,R Buchert,F Donnerstag,M Hofmann,BO Knoop,DJ Brooks,HM Emrich,WH Knapp,G Berding,K ,U Schneider,P Gielow,J Fitschen,M Stuhrmann,H Harke,R Buchert,F Donnerstag,M Hofmann,BO Knoop,DJ Brooks,HM Emrich,WH Knapp,

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[(123)I]AM281 single-photon emission computed tomography imaging of central cannabinoid CB(1) receptors before and after Delta(9)-tetrahydrocannabinol therapy and whole-body scanning for assessment of radiation dose in tourette patients. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Biological psychiatry

VOLUME: 55

Page Numbers: 904-15

Journal Abbreviation: Biol. Psychiatry

ISSN: 0006-3223

DAY: 1

MONTH: May

YEAR: 2004

[(123)I]AM281 single-photon emission computed tomography imaging of central cannabinoid CB(1) receptors before and after Delta(9)-tetrahydrocannabinol therapy and whole-body scanning for assessment of radiation dose in tourette patients. Information

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LANGUAGE: eng

NlmUniqueID: 213264

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AFFILIATION: Nuclear Medicine, University School of Medicine, Hannover, Germany.

Country: United States

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MEDLINETA: Biol Psychiatry

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