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The SPECT tracer [123I]ADAM binds selectively to serotonin transporters: a double-blind, placebo-controlled study in healthy young men.

van de Giessen E, Booij J - Eur. J. Nucl. Med. Mol. Imaging (2010)

Bottom Line: We found that specific to non-specific ratios were statistically significantly lower in paroxetine-pretreated participants than in placebo- or methylphenidate-pretreated participants.No such difference was found between groups pretreated with placebo or methylphenidate.Our preliminary findings suggest that [(123)I]ADAM binds selectively to SERTs in human brain.

View Article: PubMed Central - PubMed

Affiliation: Graduate School Neurosciences Amsterdam, Department of Nuclear Medicine, University of Amsterdam, Academic Medical Center, Amsterdam, The Netherlands.

ABSTRACT

Purpose: The tracer (123)I-2-([2-({dimethylamino}methyl)phenyl]thio)-5-iodophenylamine ([(123)I]ADAM) has been developed to image serotonin transporters (SERTs) with SPECT. Preclinical studies have shown that [(123)I]ADAM binds selectively to SERTs. Moreover, initial human studies have shown that [(123)I]ADAM binding could be blocked by selective serotonin reuptake inhibitors (SSRIs). However, in humans it has not been proven that [(123)I]ADAM binds selectively to SERTs.

Methods: We examined the in vivo availability of SERTs in 12 healthy young volunteers 5 h after bolus injection of [(123)I]ADAM. To evaluate the selectivity of binding, four participants were pretreated (double-blinded design) with placebo, four with paroxetine (20 mg) and four with the dopamine/norepinephrine blocker methylphenidate (20 mg). SPECT studies were performed on a brain-dedicated system (Neurofocus), and the SPECT images were coregistered with individual MR scans of the brain. ADAM binding in SERT-rich brain areas and cerebellar cortex (representing non-specific binding) was assessed by drawing regions of interest (ROIs) on the individual MR images. Specific to non-specific ratios were used as the outcome measure.

Results: We found that specific to non-specific ratios were statistically significantly lower in paroxetine-pretreated participants than in placebo- or methylphenidate-pretreated participants. No such difference was found between groups pretreated with placebo or methylphenidate.

Conclusion: Our preliminary findings suggest that [(123)I]ADAM binds selectively to SERTs in human brain.

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Related in: MedlinePlus

Individual and mean specific to non-specific [123I]ADAM binding ratios (BPND) in the midbrain and thalamus per pretreatment group. BPND binding potential non-displaceable
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Fig2: Individual and mean specific to non-specific [123I]ADAM binding ratios (BPND) in the midbrain and thalamus per pretreatment group. BPND binding potential non-displaceable

Mentions: The specific to non-specific ratios in the midbrain were statistically significantly lower in the group that was pretreated with paroxetine (mean ± SD: 0.24 ± 0.55) than in the placebo- (0.93 ± 0.27) or methylphenidate-pretreated group (1.13 ± 0.31; p = 0.042 and 0.043, respectively; Fig. 2). These ratios in the midbrain were not statistically significantly different between the placebo- and methylphenidate-pretreated groups (p = 0.375).Fig. 2


The SPECT tracer [123I]ADAM binds selectively to serotonin transporters: a double-blind, placebo-controlled study in healthy young men.

van de Giessen E, Booij J - Eur. J. Nucl. Med. Mol. Imaging (2010)

Individual and mean specific to non-specific [123I]ADAM binding ratios (BPND) in the midbrain and thalamus per pretreatment group. BPND binding potential non-displaceable
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2914869&req=5

Fig2: Individual and mean specific to non-specific [123I]ADAM binding ratios (BPND) in the midbrain and thalamus per pretreatment group. BPND binding potential non-displaceable
Mentions: The specific to non-specific ratios in the midbrain were statistically significantly lower in the group that was pretreated with paroxetine (mean ± SD: 0.24 ± 0.55) than in the placebo- (0.93 ± 0.27) or methylphenidate-pretreated group (1.13 ± 0.31; p = 0.042 and 0.043, respectively; Fig. 2). These ratios in the midbrain were not statistically significantly different between the placebo- and methylphenidate-pretreated groups (p = 0.375).Fig. 2

Bottom Line: We found that specific to non-specific ratios were statistically significantly lower in paroxetine-pretreated participants than in placebo- or methylphenidate-pretreated participants.No such difference was found between groups pretreated with placebo or methylphenidate.Our preliminary findings suggest that [(123)I]ADAM binds selectively to SERTs in human brain.

View Article: PubMed Central - PubMed

Affiliation: Graduate School Neurosciences Amsterdam, Department of Nuclear Medicine, University of Amsterdam, Academic Medical Center, Amsterdam, The Netherlands.

ABSTRACT

Purpose: The tracer (123)I-2-([2-({dimethylamino}methyl)phenyl]thio)-5-iodophenylamine ([(123)I]ADAM) has been developed to image serotonin transporters (SERTs) with SPECT. Preclinical studies have shown that [(123)I]ADAM binds selectively to SERTs. Moreover, initial human studies have shown that [(123)I]ADAM binding could be blocked by selective serotonin reuptake inhibitors (SSRIs). However, in humans it has not been proven that [(123)I]ADAM binds selectively to SERTs.

Methods: We examined the in vivo availability of SERTs in 12 healthy young volunteers 5 h after bolus injection of [(123)I]ADAM. To evaluate the selectivity of binding, four participants were pretreated (double-blinded design) with placebo, four with paroxetine (20 mg) and four with the dopamine/norepinephrine blocker methylphenidate (20 mg). SPECT studies were performed on a brain-dedicated system (Neurofocus), and the SPECT images were coregistered with individual MR scans of the brain. ADAM binding in SERT-rich brain areas and cerebellar cortex (representing non-specific binding) was assessed by drawing regions of interest (ROIs) on the individual MR images. Specific to non-specific ratios were used as the outcome measure.

Results: We found that specific to non-specific ratios were statistically significantly lower in paroxetine-pretreated participants than in placebo- or methylphenidate-pretreated participants. No such difference was found between groups pretreated with placebo or methylphenidate.

Conclusion: Our preliminary findings suggest that [(123)I]ADAM binds selectively to SERTs in human brain.

Show MeSH
Related in: MedlinePlus