Quantification of cortical DA receptors
with [11C]FLB 457
Background
[11C]FLB 457 (Halldin et al., 1995) is a high affinity D2/D3
receptor PET radioligand, which can be used to measure cortical (extrastriatal)
D2/D3 receptors (Olsson et al., 2004; Sudo et al., 2001; Suhara
et al., 1999; Vilkman et al., 2000).
[11C]raclopride is another much used PET radiotracer to quantify
D2/D3 receptors, but it does not provide sufficient signal-to-noise ratio
to quantify dopamine receptors in extrastriatal areas;
but then [11C]FLB 457 can not be used to quantify dopamine binding in
the striatum.
It remains controversial whether [11C]FLB 457 can also be used to
quantify cortical DA function, that is, to measure acute changes in synaptic
dopamine concentration; there are studies that support this application
(Montgomery et al., 2007; Narendran et al., 2009; Ko et al., 2009)
and studies where [11C]FLB 457 was not found suitable for this purpose
(Okauchi et al., 2001; Aalto et al., 2009).
Published analysis methods
Suggested analysis method for Turku
Reference to the articles from Turku PET Centre.
References:
Aalto S, Hirvonen J, Kaasinen V, Hagelberg N, Kajander J, Någren K, Seppälä T,
Rinne JO, Scheinin H, Hietala J.
The effects of d-amphetamine on extrastriatal dopamine
D2/D3 receptors: a randomized, double-blind,
placebo-controlled PET study with [11C]FLB 457 in
healthy subjects.
Eur J Nucl Med Mol Imaging. 2009; 36(3): 475-483.
Farde L, Suhara T, Nyberg S, Karlsson P, Nakashima Y, Hietala J, Halldin C.
A PET-study of [11C]FLB 457 binding to extrastriatal D2-dopamine
receptors in healthy subjects and antipsychotic drug-treated patients.
Psychopharmacology (Berl). 1997; 133(4): 396-404.
Hagelberg N, Aalto S, Kajander J, Oikonen V, Hinkka S, Någren K, Hietala J,
Scheinin H. Alfentanil increases cortical dopamine D2/D3
receptor binding in healthy subjects.
Pain 2004; 109(1-2): 86-93.
Halldin C, Farde L, Högberg T, Mohell N, Hall H, Suhara T, Karlsson
P, Nakashima Y, Swahn CG. 1995. Carbon-11-FLB 457: A radioligand
for extrastriatal D2 dopamine receptors. J Nucl Med. 1995;
36: 1275–1281.
Ikoma Y, Ito H, Arakawa R, Okumura M, Seki C, Shidahara M, Takahashi H,
Kimura Y, Kanno I, Suhara T.
Error analysis for PET measurement of dopamine D2 receptor occupancy
by antipsychotics with [11C]raclopride and [11C]FLB 457.
Neuroimage 2008; 42(4): 1285-1294.
Ito H, Sudo Y, Suhara T, Okubo Y, Halldin C, Farde L.
Error analysis for quantification of [11C]FLB 457 binding to
extrastriatal D2 dopamine receptors in the human brain.
Neuroimage 2001; 13(3):531-539.
Kaasinen V, Vilkman H, Hietala J, Någren K, Helenius H, Olsson H, Farde L,
Rinne J. Age-related dopamine D2/D3 receptor loss in
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Ko JH, Ptito A, Monchi O, Cho SS, Van Eimeren T, Pellecchia G, Ballanger B,
Rusjan P, Houle S, Strafella AP. Increased dopamine release in the rightanterior cingulate cortex during the performance of a sorting task:
A [11C]FLB 457 PET study. Neuroimage 2009; 46: 516-521.
Montgomery AJ, Asselin MC, Farde L, Grasby PM.
Measurement of methylphenidate-induced change in extrastriatal dopamine
concentration using [11C]FLB 457 PET.
J Cereb Blood Flow Metab. 2007; 27(2): 369-377.
Narendran R, Frankle WG, Mason NS, Rabiner EA, Gunn RN, Searle GE, Vora S,
Litschge M, Kendro S, Cooper TB, Mathis CA, Laruelle M.
Positron emission tomography imaging of amphetamine-induced dopamine release in
the human cortex: A comparative evaluation of the high affinity dopamine
D2/3 radiotracers [11C]FLB 457 and
[11C]fallypride. Synapse 2009; 63(6): 447-461.
Okauchi T, Suhara T, Maeda J, Kawabe K, Obayashi S, Suzuki K.
Effect of endogenous dopamine on endogenous dopamine on extrastriated
[11C]FLB 457 binding measured by PET.
Synapse 2001; 41(2): 87-95.
Okubo Y, Olsson H, Ito H, Lofti M, Suhara T, Halldin C, Farde L.
PET mapping of extrastriatal D2-like dopamine receptors in the human
brain using an anatomic standardization technique and [11C]FLB 457.
Neuroimage 1999; 10(6): 666-674.
Olsson H, Halldin C, Swahn CG, Farde L.
Quantification of [11C]FLB 457 binding to extrastriatal dopamine
receptors in the human brain.
J Cereb Blood Flow Metab. 1999; 19(10): 1164-1173.
Sudo Y, Suhara T, Inoue M, Ito H, Suzuki K, Saijo T, Halldin C, Farde L.
Reproducibility of [11C]FLB 457 binding in extrastriatal regions.
Nucl Med Commun. 2001; 22(11): 1215-1221.
Suhara T, Sudo Y, Okauchi T, Maeda J, Kawabe K, Suzuki K, Okubo Y,
Nakashima Y, Ito H, Tanada S, Halldin C, Farde L.
Extrastriatal dopamine D2 receptor density and affinity in
the human brain measured by 3D PET.
Int J Neuropsychopharmacol. 1999; 2(2): 73-82.
Vilkman H, Kajander J, Någren K, Oikonen V, Syvälahti E, Hietala J.
Measurement of extrastriatal D2-like receptor binding with
[11C]FLB 457 - a test-retest analysis.
Eur J Nucl Med. 2000; 27(11): 1666-1673.
