Quantification of cortical DA receptors with [11C]FLB 457 (draft)

[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 radioligand 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, 2013, and 2014; 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).

Suggested analysis method for Turku

Please read the articles from Turku PET Centre.

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Asselin MC, Montgomery AJ, Grasby PM, Hume SP. Quantification of PET studies with the very high-affinity dopamine D2/D3 receptor ligand [11C]FLB 457: re-evaluation of the validity of using a cerebellar reference region. J Cereb Blood Flow Metab. 2007; 27(2): 378-392. doi: 10.1038/sj.jcbfm.9600340.

Cselényi Z, Olsson H, Halldin C, Gulyás B, Farde L. A comparison of recent parametric neuroreceptor mapping approaches based on measurements with the high affinity PET radioligands [11C]FLB 457 and [11C]WAY 100635. Neuroimage 2006; 32: 1690-1708. doi: 10.1016/j.neuroimage.2006.02.053.

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. doi: 10.1007/s002130050420.

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. doi: 10.1016/j.pain.2004.01.013.

Hirvonen MM, Lumme V, Hirvonen J, Pesonen U, Någren K, Vahlberg T, Scheinin H, Hietala J. C957T polymorphism of the human dopamine D2 receptor gene predicts extrastriatal dopamine receptor availability in vivo. Prog Neuropsychopharmacol Biol Psychiatry 2009; 33(4): 630-636. doi: 10.1016/j.pnpbp.2009.02.021.

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. doi: 10.1016/j.neuroimage.2008.05.056.

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. doi: 10.1006/nimg.2000.0717.

Kaasinen V, Vilkman H, Hietala J, Någren K, Helenius H, Olsson H, Farde L, Rinne J. Age-related dopamine D2/D3 receptor loss in extrastriatal regions of the human brain. Neurobiol Aging. 2000; 21(5): 683-638. doi: 10.1016/s0197-4580(00)00149-4.

Narendran R, Mason NS, May MA, Chen CM, Kendro S, Ridler K, Rabiner EA, Laruelle M, Mathis CA, Frankle WG. Positron emission tomography imaging of dopamine D2/3 receptors in the human cortex with [11C]FLB 457: reproducibility studies. Synapse 2011; 65(1): 35-40. doi: 10.1002/syn.20813.

Narendran R, Mason NS, Chen CM, Himes M, Keating P, May MA, Rabiner EA, Laruelle M, Mathis CA, Frankle WG. Evaluation of dopamine D2/3 specific binding in the cerebellum for the positron emission tomography radiotracer [11C]FLB 457: implications for measuring cortical dopamine release. Synapse 2011; 65(10): 991-997. doi: 10.1002/syn.20926.

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. doi: 10.1006/nimg.1999.0502.

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. doi: 10.1097/00004647-199910000-00013.

Olsson H, Farde L. Potentials and pitfalls using high affinity radioligands in PET and SPET determinations on regional drug induced D2 receptor occupancy - a simulation study based on experimental data. Neuroimage 2001; 14(4): 936-945. doi: 10.1006/nimg.2001.0879.

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. doi: 10.1007/s002590000342.

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Updated at: 2014-10-08
Created at: 2007-12-03
Written by: Vesa Oikonen