Reproducibility of in vivo brain measures of 5-HT2A receptors with PET and [18F]deuteroaltanserin

Soares, Jair C.; Dyck, Christopher H. van; Tan, Ping‐Zhong; Zoghbi, Sami S.; Garg, Pradeep; Soufer, Robert; Baldwin, Ronald M.; Fujita, Masahiro; Staley, Julie K.; Fu, Xun; Amici, Louis; Seibyl, John; Innis, Robert B.

doi:10.1016/s0925-4927(01)00071-3

Cited by 17 publications

(11 citation statements)

References 22 publications

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“…In humans, cortical‐to‐cerebellar ratio was increased by 26% above that observed previously for [ 18 F]altanserin, suggesting it might be a superior PET radioligand . In a subsequent study by the same group, the test–retest reliability was also quite good …”

Section: Current Radioligands For Imaging the 5‐ht Systemmentioning

confidence: 51%

5‐HT radioligands for human brain imaging with PET and SPECT

Paterson

Kornum

Nutt

et al. 2011

Medicinal Research Reviews

145

129

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The serotonergic system plays a key modulatory role in the brain and is the target for many drug treatments for brain disorders either through reuptake blockade or via interactions at the 14 subtypes of 5-HT receptors. This review provides the history and current status of radioligands used for positron emission tomography (PET) and single photon emission computerized tomography (SPECT) imaging of human brain serotonin (5-HT) receptors, the 5-HT transporter (SERT), and 5-HT synthesis rate. Currently available radioligands for in vivo brain imaging of the 5-HT system in humans include antagonists for the 5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4 receptors, and for SERT. Here we describe the evolution of these radioligands, along with the attempts made to develop radioligands for additional serotonergic targets. We describe the properties needed for a radioligand to become successful and the main caveats. The success of a PET or SPECT radioligand can ultimately be assessed by its frequency of use, its utility in humans, and the number of research sites using it relative to its invention date, and so these aspects are also covered. In conclusion, the development of PET and SPECT radioligands to image serotonergic targets is of high interest, and successful evaluation in humans is leading to invaluable insight into normal and abnormal brain function, emphasizing the need for continued development of both SPECT and PET radioligands for human brain imaging.

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Section: Current Radioligands For Imaging the 5‐ht Systemmentioning

confidence: 51%

5‐HT radioligands for human brain imaging with PET and SPECT

Paterson

Kornum

Nutt

et al. 2011

Medicinal Research Reviews

145

129

View full text Add to dashboard Cite

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“…The replacement of hydrogen with deuterium in [ 18 F]altanserin reduces the rate of undesirable radiometabolite formation. [ 18 F]deuteroaltanserin shows better characteristics and 26% higher brain uptake than [ 18 F]altanserin itself in nonhuman primates and human [102, 103]. Although higher binding in estrogen replacement and lower binding in cortical regions of AD are reported using [ 18 F]deuteroaltanserin, not many studies are available at present to thoroughly assess its potential [104].…”

Section: Introductionmentioning

confidence: 99%

PET Tracers for Serotonin Receptors and Their Applications

Js¹,

Mann

2015

CNSAMC

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Serotonin receptors (5-HTRs) are implicated in the pathophysiology of a variety of neuropsychiatric and neurodegenerative disorders and are also targets for drug therapy. In the CNS, most of these receptors are expressed in high abundance in specific brain regions reflecting their role in brain functions. Quantifying binding to 5-HTRs in vivo may permit assessment of physiologic and pathologic conditions, and monitoring disease progression, evaluating treatment response, and for investigating new treatment modalities. Positron emission tomography (PET) molecular imaging has the sensitivity to quantify binding of 5-HTRs in CNS disorders and to measure drug occupancy as part of a process of new drug development. Although research on PET imaging of 5-HTRs have been performed more than two decades, the successful radiotracers so far

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“…The radiotracers [ 18 F]-altanserin, [ 11 C]-MDL100,907, and [ 18 F]-setoperone have been used to study cortical 5HT 2A R in neurochemical PET imaging studies [12,14,16-21]. Test-retest variability of 5HT 2A R measurement with [ 18 F]-altanserin and PET with arterial blood sampling has been reported in several studies.…”

Section: Introductionmentioning

confidence: 99%

“…Test-retest variability of 5HT 2A R measurement with [ 18 F]-altanserin and PET with arterial blood sampling has been reported in several studies. Soares et al reported high mean intra-subject % change of 11–14% for cortical brain areas for the ratio of specific to non-displaceable brain uptakes and the ratio of specific brain uptake to total parent plasma concentration [21]. A four compartment mode tracer kinetic model yielded average differences of 13% or less in regions of high receptor concentrations and 16–20% for regions of low receptor concentrations.…”

Section: Introductionmentioning

confidence: 99%

Test-retest variability of high resolution positron emission tomography (PET) imaging of cortical serotonin (5HT2A) receptors in older, healthy adults

et al. 2009

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BackgroundPosition emission tomography (PET) imaging using [18F]-setoperone to quantify cortical 5-HT2A receptors has the potential to inform pharmacological treatments for geriatric depression and dementia. Prior reports indicate a significant normal aging effect on serotonin 5HT2A receptor (5HT2AR) binding potential. The purpose of this study was to assess the test-retest variability of [18F]-setoperone PET with a high resolution scanner (HRRT) for measuring 5HT2AR availability in subjects greater than 60 years old. Methods: Six healthy subjects (age range = 65–78 years) completed two [18F]-setoperone PET scans on two separate occasions 5–16 weeks apart.ResultsThe average difference in the binding potential (BPND) as measured on the two occasions in the frontal and temporal cortical regions ranged between 2 and 12%, with the lowest intraclass correlation coefficient in anterior cingulate regions.ConclusionWe conclude that the test-retest variability of [18F]-setoperone PET in elderly subjects is comparable to that of [18F]-setoperone and other 5HT2AR radiotracers in younger subject samples.

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Reproducibility of in vivo brain measures of 5-HT2A receptors with PET and [18F]deuteroaltanserin

Cited by 17 publications

References 22 publications

5‐HT radioligands for human brain imaging with PET and SPECT

5‐HT radioligands for human brain imaging with PET and SPECT

PET Tracers for Serotonin Receptors and Their Applications

Test-retest variability of high resolution positron emission tomography (PET) imaging of cortical serotonin (5HT2A) receptors in older, healthy adults

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