[11C]NNC 112 selectivity for dopamine D1 and serotonin 5-HT(2A) receptors: a PET study in healthy human subjects.

Full Abstract

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.

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Author information

Author/s: Slifstein, Mark (M); Kegeles, Lawrence S (LS); Gonzales, Robyn (R); Frankle, William G (WG); Xu, Xiaoyan (X); Laruelle, Marc (M); Abi-Dargham, Anissa (A);

Affiliation: Department of Psychiatry, Columbia University, New York, New York, USA. mms218(-atsign-)columbia.edu

Grants: MH0661710-03 (Agency:NIMH NIH HHS)

Journal and publication information

Publication Type: Journal Article; Research Support, N.I.H., Extramural

Journal: Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism (J Cereb Blood Flow Metab), published in United States. (Language: eng)

Reference: 2007-Oct; vol 27 (issue 10) : pp 1733-41

Dates: Created 2007/09/20; Completed 2007/10/17; Revised 2007/12/03;

PMID: 17311076, status: MEDLINE (last retrieval date: 12/26/2008)

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MeSH headings (categories)

This article was linked to the MESH Headings shown below.

Adult
Benzazepines - pharmacology
Benzofurans - pharmacology
Brain - metabolism
Female
Health

Humans
Male
Positron-Emission Tomography
Receptors, Dopamine D1 - metabolism
Receptors, Serotonin - metabolism
Risperidone - pharmacology

Associated Chemicals: Benzazepines (0) ; Benzofurans (0) ; Receptors, Dopamine D1 (0) ; Receptors, Serotonin (0) ; Risperidone (106266-06-2) ; NNC 112 (125341-24-4)

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