No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human
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No change in [¹¹C]CUMI-101 binding to 5-HT(1A) receptors after intravenous citalopram in human. / Pinborg, Lars H; Feng, Ling; Haahr, Mette E; Gillings, Nic; Dyssegaard, Agnete; Madsen, Jacob; Svarer, Claus; Yndgaard, Stig; Kjaer, Troels W; Parsey, Ramin V; Hansen, Hanne D; Ettrup, Anders; Paulson, Olaf B; Knudsen, Gitte M.
In: Synapse, Vol. 66, No. 10, 10.2012, p. 880-4.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
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
N1 - Copyright © 2012 Wiley Periodicals, Inc.
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.
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.
U2 - 10.1002/syn.21579
DO - 10.1002/syn.21579
M3 - Journal article
VL - 66
SP - 880
EP - 884
JO - Synapse
JF - Synapse
SN - 0887-4476
IS - 10
ER -
ID: 48555379