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Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36

Research output: Research - peer-reviewJournal article

Standard

Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36. / Ettrup, A.; da Cunha-Bang, S.; McMahon, Barry P.; Lehel, S.; Dyssegaard, A.; Skibsted, A.W.; Jørgensen, Louise Møller; Hansen, M.; Baandrup, A.O.; Bache, S.; Svarer, C.; Kristensen, Jesper Langgaard; Gillings, N.; Madsen, Jacob; Knudsen, G.M.

In: Journal of Cerebral Blood Flow and Metabolism, Vol. 34, 30.04.2014, p. 1188-1196.

Research output: Research - peer-reviewJournal article

Harvard

Ettrup, A, da Cunha-Bang, S, McMahon, BP, Lehel, S, Dyssegaard, A, Skibsted, AW, Jørgensen, LM, Hansen, M, Baandrup, AO, Bache, S, Svarer, C, Kristensen, JL, Gillings, N, Madsen, J & Knudsen, GM 2014, 'Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36' Journal of Cerebral Blood Flow and Metabolism, vol 34, pp. 1188-1196. DOI: 10.1038/jcbfm.2014.68

APA

Ettrup, A., da Cunha-Bang, S., McMahon, B. P., Lehel, S., Dyssegaard, A., Skibsted, A. W., ... Knudsen, G. M. (2014). Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36. Journal of Cerebral Blood Flow and Metabolism, 34, 1188-1196. DOI: 10.1038/jcbfm.2014.68

Vancouver

Ettrup A, da Cunha-Bang S, McMahon BP, Lehel S, Dyssegaard A, Skibsted AW et al. Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36. Journal of Cerebral Blood Flow and Metabolism. 2014 Apr 30;34:1188-1196. Available from, DOI: 10.1038/jcbfm.2014.68

Author

Ettrup, A. ; da Cunha-Bang, S. ; McMahon, Barry P. ; Lehel, S. ; Dyssegaard, A. ; Skibsted, A.W. ; Jørgensen, Louise Møller ; Hansen, M. ; Baandrup, A.O. ; Bache, S. ; Svarer, C. ; Kristensen, Jesper Langgaard ; Gillings, N. ; Madsen, Jacob ; Knudsen, G.M./ Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36. In: Journal of Cerebral Blood Flow and Metabolism. 2014 ; Vol. 34. pp. 1188-1196

Bibtex

@article{56b24e8ba27448f69f7350cc065b2a35,
title = "Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36",
abstract = "[C]Cimbi-36 was recently developed as a selective serotonin 2A (5-HT) receptor agonist radioligand for positron emission tomography (PET) brain imaging. Such an agonist PET radioligand may provide a novel, and more functional, measure of the serotonergic system and agonist binding is more likely than antagonist binding to reflect 5-HT levels in vivo. Here, we show data from a first-in-human clinical trial with [C]Cimbi-36. In 29 healthy volunteers, we found high brain uptake and distribution according to 5-HT receptors with [C]Cimbi-36 PET. The two-tissue compartment model using arterial input measurements provided the most optimal quantification of cerebral [C]Cimbi-36 binding. Reference tissue modeling was feasible as it induced a negative but predictable bias in [C]Cimbi-36 PET outcome measures. In five subjects, pretreatment with the 5-HT receptor antagonist ketanserin before a second PET scan significantly decreased [C]Cimbi-36 binding in all cortical regions with no effects in cerebellum. These results confirm that [C]Cimbi-36 binding is selective for 5-HT receptors in the cerebral cortex and that cerebellum is an appropriate reference tissue for quantification of 5-HT receptors in the human brain. Thus, we here describe [C]Cimbi-36 as the first agonist PET radioligand to successfully image and quantify 5-HT receptors in the human brain.Journal of Cerebral Blood Flow & Metabolism advance online publication, 30 April 2014; doi:10.1038/jcbfm.2014.68.",
author = "A. Ettrup and {da Cunha-Bang}, S. and McMahon, {Barry P.} and S. Lehel and A. Dyssegaard and A.W. Skibsted and Jørgensen, {Louise Møller} and M. Hansen and A.O. Baandrup and S. Bache and C. Svarer and Kristensen, {Jesper Langgaard} and N. Gillings and Jacob Madsen and G.M. Knudsen",
year = "2014",
month = "4",
doi = "10.1038/jcbfm.2014.68",
volume = "34",
pages = "1188--1196",
journal = "Journal of Cerebral Blood Flow and Metabolism",
issn = "0271-678X",
publisher = "Sage Publications Ltd.",

}

RIS

TY - JOUR

T1 - Serotonin 2A receptor agonist binding in the human brain with [C]Cimbi-36

AU - Ettrup,A.

AU - da Cunha-Bang,S.

AU - McMahon,Barry P.

AU - Lehel,S.

AU - Dyssegaard,A.

AU - Skibsted,A.W.

AU - Jørgensen,Louise Møller

AU - Hansen,M.

AU - Baandrup,A.O.

AU - Bache,S.

AU - Svarer,C.

AU - Kristensen,Jesper Langgaard

AU - Gillings,N.

AU - Madsen,Jacob

AU - Knudsen,G.M.

PY - 2014/4/30

Y1 - 2014/4/30

N2 - [C]Cimbi-36 was recently developed as a selective serotonin 2A (5-HT) receptor agonist radioligand for positron emission tomography (PET) brain imaging. Such an agonist PET radioligand may provide a novel, and more functional, measure of the serotonergic system and agonist binding is more likely than antagonist binding to reflect 5-HT levels in vivo. Here, we show data from a first-in-human clinical trial with [C]Cimbi-36. In 29 healthy volunteers, we found high brain uptake and distribution according to 5-HT receptors with [C]Cimbi-36 PET. The two-tissue compartment model using arterial input measurements provided the most optimal quantification of cerebral [C]Cimbi-36 binding. Reference tissue modeling was feasible as it induced a negative but predictable bias in [C]Cimbi-36 PET outcome measures. In five subjects, pretreatment with the 5-HT receptor antagonist ketanserin before a second PET scan significantly decreased [C]Cimbi-36 binding in all cortical regions with no effects in cerebellum. These results confirm that [C]Cimbi-36 binding is selective for 5-HT receptors in the cerebral cortex and that cerebellum is an appropriate reference tissue for quantification of 5-HT receptors in the human brain. Thus, we here describe [C]Cimbi-36 as the first agonist PET radioligand to successfully image and quantify 5-HT receptors in the human brain.Journal of Cerebral Blood Flow & Metabolism advance online publication, 30 April 2014; doi:10.1038/jcbfm.2014.68.

AB - [C]Cimbi-36 was recently developed as a selective serotonin 2A (5-HT) receptor agonist radioligand for positron emission tomography (PET) brain imaging. Such an agonist PET radioligand may provide a novel, and more functional, measure of the serotonergic system and agonist binding is more likely than antagonist binding to reflect 5-HT levels in vivo. Here, we show data from a first-in-human clinical trial with [C]Cimbi-36. In 29 healthy volunteers, we found high brain uptake and distribution according to 5-HT receptors with [C]Cimbi-36 PET. The two-tissue compartment model using arterial input measurements provided the most optimal quantification of cerebral [C]Cimbi-36 binding. Reference tissue modeling was feasible as it induced a negative but predictable bias in [C]Cimbi-36 PET outcome measures. In five subjects, pretreatment with the 5-HT receptor antagonist ketanserin before a second PET scan significantly decreased [C]Cimbi-36 binding in all cortical regions with no effects in cerebellum. These results confirm that [C]Cimbi-36 binding is selective for 5-HT receptors in the cerebral cortex and that cerebellum is an appropriate reference tissue for quantification of 5-HT receptors in the human brain. Thus, we here describe [C]Cimbi-36 as the first agonist PET radioligand to successfully image and quantify 5-HT receptors in the human brain.Journal of Cerebral Blood Flow & Metabolism advance online publication, 30 April 2014; doi:10.1038/jcbfm.2014.68.

UR - http://www.scopus.com/inward/record.url?scp=84898731075&partnerID=8YFLogxK

U2 - 10.1038/jcbfm.2014.68

DO - 10.1038/jcbfm.2014.68

M3 - Journal article

VL - 34

SP - 1188

EP - 1196

JO - Journal of Cerebral Blood Flow and Metabolism

T2 - Journal of Cerebral Blood Flow and Metabolism

JF - Journal of Cerebral Blood Flow and Metabolism

SN - 0271-678X

ER -

ID: 111037056