Analysis of [18F]deuteroaltanserin PET data

[18F]altanserin is an excellent radioligand for studying the density of serotonin 5-HT2A receptors, except that its BBB-penetrating radiometabolite requires a relatively long bolus-infusion study protocol (Paterson et al., 2013). Substitution of two deuterium atoms for hydrogen atoms retards the metabolism, leading to improved target-to-background ratio (Tan et al., 1998; van Dyck et al., 2000). Bolus-infusion protocol was still feasible for [18F]deuteroaltanserin, providing again excellent test-retest reproducibility (van Dyck et al., 2000; Soares et al., 2001; Staley et al., 2001). The dynamic PET scan is started about 5 h after the start of bolus-infusion (van Dyck et al., 2000; Kugaya et al., 2003; Santhosh et al., 2009).


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References:

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Kugaya A, Epperson CN, Zoghbi S, van Dyck CH, Hou Y, Fujita M, Staley JK, Garg PK, Seibyl JP, Innis RB. Increase in prefrontal cortex serotonin 2A receptors following estrogen treatment in postmenopausal women. Am J Psychiatry 2003; 160: 1522–1524.

Paterson LM, Kornum BR, Nutt DJ, Pike VW, Knudsen GM. 5-HT radioligands for human brain imaging with PET and SPECT. Med Res Rev. 2013; 33(1): 54-111.

Santhosh L, Estok KM, Vogel RS, Tamagnan GD, Baldwin RM, Mitsis EM, Macavoy MG, Staley JK, van Dyck CH. Regional distribution and behavioral correlates of 5-HT2A receptors in Alzheimer’s disease with [18F]deuteroaltanserin and PET. Psychiatry Res. 2009; 173: 212–217.

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Staley JK, Van Dyck CH, Tan PZ, Al Tikriti M, Ramsby Q, Klump H, Ng C, Garg P, Soufer R, Baldwin RM, Innis RB. Comparison of [18F]altanserin and [18)F]deuteroaltanserin for PET imaging of serotonin2A receptors in baboon brain: pharmacological studies. Nucl Med Biol. 2001; 28: 271–279.

Tan P-Z, Soares J, Baldwin RM, van Dyck CH, Soufer R, Seibyl JP, Charney DS, Innis RB. H-2 and F-18 dual-labeled altanserin as a metabolically resistant PET ligand for serotonin-2A (5-HT2A) receptor. J Nucl Med. 1998; 39, 21P.

van Dyck CH, Soares JC, Tan PZ, Staley JK, Baldwin RM, Amici LA, Fu X, Garg PK, Seibyl JP, Charney DS, Innis RB. Equilibrium modeling of 5-HT2A receptors with [18F]deuteroaltanserin and PET: Feasibility of a constant infusion paradigm. Nucl Med Biol. 2000; 27: 715–722.



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Created at: 2016-08-23
Updated at: 2016-08-24
Written by: Vesa Oikonen