No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human

Lars H Pinborg; Ling Feng; Mette E Haahr; Nic Gillings; Agnete Dyssegaard; Jacob Madsen; Claus Svarer; Stig Yndgaard; Troels W Kjaer; Ramin V Parsey; Hanne D Hansen; Anders Ettrup; Olaf B Paulson; Gitte M Knudsen

doi:10.1002/syn.21579

No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human

Lars H Pinborg, Ling Feng, Mette E Haahr, Nic Gillings, Agnete Dyssegaard, Jacob Madsen, Claus Svarer, Stig Yndgaard, Troels W Kjaer, Ramin V Parsey, Hanne D Hansen, Anders Ettrup, Olaf B Paulson, Gitte M Knudsen

27 Citations (Scopus)

Abstract

The main objective of this study was to determine the sensitivity of [ ¹¹C]CUMI-101 to citalopram challenge aiming at increasing extracellular 5-HT. CUMI-101 has agonistic properties in human embryonic kidney 293 cells transfected with human recombinant 5-HT _1A receptors (Hendry et al. [2011] Nucl Med Biol 38:273-277; Kumar et al. [2006] J Med Chem 49:125-134) and has previously been demonstrated to be sensitive to bolus citalopram in monkeys (Milak et al. [2011] J Cereb Blood Flow Metab 31:243-249). We studied six healthy individuals. Two PET-scans were performed on the same day in each individual before and after constant infusion of citalopram (0.15 mg/kg). The imaging data were analyzed using two tissue compartment kinetic modeling with metabolite corrected arterial input and Simplified Reference Tissue Modeling using cerebellum as a reference region. There was no significant difference in regional distribution volume or non-displaceable binding potential values before and after citalopram infusion. The mean receptor occupancy was 0.03 (range -0.14 to 0.17). Our data imply that [ ¹¹C]CUMI-101 binding is not sensitive to citalopram infusion in humans. Synapse, 2012.

Original language	English
Journal	Synapse
Volume	66
Issue number	10
Pages (from-to)	880-4
Number of pages	5
ISSN	0887-4476
DOIs	https://doi.org/10.1002/syn.21579
Publication status	Published - Oct 2012

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@article{4e9c7acdeca7421d883263b0cdd7b086,

title = "No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human",

abstract = "The main objective of this study was to determine the sensitivity of [ 11C]CUMI-101 to citalopram challenge aiming at increasing extracellular 5-HT. CUMI-101 has agonistic properties in human embryonic kidney 293 cells transfected with human recombinant 5-HT 1A receptors (Hendry et al. [2011] Nucl Med Biol 38:273-277; Kumar et al. [2006] J Med Chem 49:125-134) and has previously been demonstrated to be sensitive to bolus citalopram in monkeys (Milak et al. [2011] J Cereb Blood Flow Metab 31:243-249). We studied six healthy individuals. Two PET-scans were performed on the same day in each individual before and after constant infusion of citalopram (0.15 mg/kg). The imaging data were analyzed using two tissue compartment kinetic modeling with metabolite corrected arterial input and Simplified Reference Tissue Modeling using cerebellum as a reference region. There was no significant difference in regional distribution volume or non-displaceable binding potential values before and after citalopram infusion. The mean receptor occupancy was 0.03 (range -0.14 to 0.17). Our data imply that [ 11C]CUMI-101 binding is not sensitive to citalopram infusion in humans. Synapse, 2012.",

author = "Pinborg, {Lars H} and Ling Feng and Haahr, {Mette E} and Nic Gillings and Agnete Dyssegaard and Jacob Madsen and Claus Svarer and Stig Yndgaard and Kjaer, {Troels W} and Parsey, {Ramin V} and Hansen, {Hanne D} and Anders Ettrup and Paulson, {Olaf B} and Knudsen, {Gitte M}",

note = "Copyright {\textcopyright} 2012 Wiley Periodicals, Inc.",

year = "2012",

month = oct,

doi = "10.1002/syn.21579",

language = "English",

volume = "66",

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T1 - No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human

AU - Pinborg, Lars H

AU - Feng, Ling

AU - Haahr, Mette E

AU - Gillings, Nic

AU - Dyssegaard, Agnete

AU - Madsen, Jacob

AU - Svarer, Claus

AU - Yndgaard, Stig

AU - Kjaer, Troels W

AU - Parsey, Ramin V

AU - Hansen, Hanne D

AU - Ettrup, Anders

AU - Paulson, Olaf B

AU - Knudsen, Gitte M

PY - 2012/10

Y1 - 2012/10

N2 - The main objective of this study was to determine the sensitivity of [ 11C]CUMI-101 to citalopram challenge aiming at increasing extracellular 5-HT. CUMI-101 has agonistic properties in human embryonic kidney 293 cells transfected with human recombinant 5-HT 1A receptors (Hendry et al. [2011] Nucl Med Biol 38:273-277; Kumar et al. [2006] J Med Chem 49:125-134) and has previously been demonstrated to be sensitive to bolus citalopram in monkeys (Milak et al. [2011] J Cereb Blood Flow Metab 31:243-249). We studied six healthy individuals. Two PET-scans were performed on the same day in each individual before and after constant infusion of citalopram (0.15 mg/kg). The imaging data were analyzed using two tissue compartment kinetic modeling with metabolite corrected arterial input and Simplified Reference Tissue Modeling using cerebellum as a reference region. There was no significant difference in regional distribution volume or non-displaceable binding potential values before and after citalopram infusion. The mean receptor occupancy was 0.03 (range -0.14 to 0.17). Our data imply that [ 11C]CUMI-101 binding is not sensitive to citalopram infusion in humans. Synapse, 2012.

AB - The main objective of this study was to determine the sensitivity of [ 11C]CUMI-101 to citalopram challenge aiming at increasing extracellular 5-HT. CUMI-101 has agonistic properties in human embryonic kidney 293 cells transfected with human recombinant 5-HT 1A receptors (Hendry et al. [2011] Nucl Med Biol 38:273-277; Kumar et al. [2006] J Med Chem 49:125-134) and has previously been demonstrated to be sensitive to bolus citalopram in monkeys (Milak et al. [2011] J Cereb Blood Flow Metab 31:243-249). We studied six healthy individuals. Two PET-scans were performed on the same day in each individual before and after constant infusion of citalopram (0.15 mg/kg). The imaging data were analyzed using two tissue compartment kinetic modeling with metabolite corrected arterial input and Simplified Reference Tissue Modeling using cerebellum as a reference region. There was no significant difference in regional distribution volume or non-displaceable binding potential values before and after citalopram infusion. The mean receptor occupancy was 0.03 (range -0.14 to 0.17). Our data imply that [ 11C]CUMI-101 binding is not sensitive to citalopram infusion in humans. Synapse, 2012.

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DO - 10.1002/syn.21579

M3 - Journal article

SN - 0887-4476

VL - 66

SP - 880

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JO - Synapse

JF - Synapse

IS - 10

ER -

No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human

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