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. Author manuscript; available in PMC: 2014 Oct 7.
Published in final edited form as: Med Res Rev. 2011 Jun 14;33(1):54–111. doi: 10.1002/med.20245

Table III.

Successful and Promising PET and SPECT Radioligands for Serotonergic Targets in Humans

Target Radioligand First in man Animal studies Human studies Research institutions
5-HT1A [11C]WAY-100635 1995 10 80 12
[18F]MPPF 2000 27 21 6
[18F]FCWAY 2000 7 11 1
[11C]CUMI-101 2008a 2 1a 1
5-HT1B [11C]AZ10419369 2008 3 1 1
[11C]P943 2009 1 3 1
5-HT2A [123I]-5-I-R91150 1997 9 19 6
[18F]setoperoneb 1990 3 36 7
[18F]altanserin 1994 5 51 10
[18F]deuteroaltanserin 1998 2a 5a 1
[11C]MDL100907 1998 5 6 5
5-HT4 [11C]SB207145 2008 3a 3a 2
5-HT6 [11C]GSK215083 2008 1 2 1
SERT Beta-[123I]CITb 1993 20 87 18
[123I]ADAM 2005 11 28 12
[11C]DASB 2000 17 48 16
[11C]MADAM 2005 1 7 2
5-HT synthesis [11C]-AMT 1997 2c 17d 2
[11C]-HTP 1991 4 10 3

“First in man” indicates the year when the tracer was first tested inhuman subjects as determined from publication of full papers or conference proceedings. “Animal studies” indicate the number of published manuscripts that include data from any animal species other than humans; these include ex vivo, SPECT, and/or PET studies in rat, cat, pig, dog, or nonhuman primate. “Human studies” indicate the number of PET or SPECT published manuscripts.

a

Publications may also include conference proceedings. “Research institutions” indicates the number of centers using the tracer in human subjects. The number of publications and research institutions indicated are correct at the time of writing (July 2010).

b

Tracer has multiple binding sites but only those reporting on the serotonergic target of interest are included.

c

Many animal studies have been performed with the carbon-14 equivalent of this tracer but these are not listed here.

d

Majority of studies are measuring kynurenine metabolism in tumors rather than 5-HTsynthesis per se.