Document Detail

[11C]NNC 112 selectivity for dopamine D1 and serotonin 5-HT(2A) receptors: a PET study in healthy human subjects.
MedLine Citation:
PMID:  17311076     Owner:  NLM     Status:  MEDLINE    
The dopamine D(1) receptor antagonist radioligand [(11)C]NNC 112 has previously been reported to have 100-fold selectivity for the D(1) receptor compared with the serotonin 5-HT(2A) receptor. In this study, we tested the selectivity by scanning seven healthy human research volunteers with [(11)C]NNC 112 before and after 2 mg of the antipsychotic drug risperidone, a dose that putatively blocks all 5-HT(2A) receptors with negligible effect on D(1) receptors. We found that specific binding in cortical regions was reduced by 20% to 30%, whereas the striatum showed no change. Based on the known relative densities of these receptors in humans, our results suggest 5- to 10-fold selectivity of [(11)C]NNC 112 for D(1) versus 5-HT(2A) as opposed to 100-fold selectivity. These results suggest caution in interpreting data from studies using this tracer to measure cortical D(1) receptors as well as the need for more selective radioligands to assess cortical D(1) receptors.
Mark Slifstein; Lawrence S Kegeles; Robyn Gonzales; William G Frankle; Xiaoyan Xu; Marc Laruelle; Anissa Abi-Dargham
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural     Date:  2007-02-21
Journal Detail:
Title:  Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism     Volume:  27     ISSN:  0271-678X     ISO Abbreviation:  J. Cereb. Blood Flow Metab.     Publication Date:  2007 Oct 
Date Detail:
Created Date:  2007-09-20     Completed Date:  2007-10-17     Revised Date:  2007-12-03    
Medline Journal Info:
Nlm Unique ID:  8112566     Medline TA:  J Cereb Blood Flow Metab     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1733-41     Citation Subset:  IM    
Department of Psychiatry, Columbia University, New York, New York, USA.
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MeSH Terms
Benzazepines / pharmacology*
Benzofurans / pharmacology*
Brain / metabolism
Positron-Emission Tomography
Receptors, Dopamine D1 / metabolism*
Receptors, Serotonin / metabolism*
Risperidone / pharmacology
Grant Support
MH0661710-03/MH/NIMH NIH HHS
Reg. No./Substance:
0/Benzazepines; 0/Benzofurans; 0/Receptors, Dopamine D1; 0/Receptors, Serotonin; 106266-06-2/Risperidone; 125341-24-4/NNC 112

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