Synthesis and in vivo evaluation of [O‐methyl‐11C] 2‐(4‐methoxyphenyl)‐N‐(4‐methylbenzyl)‐N‐(1‐methyl‐ piperidin‐4‐yl)acetamide as an imaging probe for 5‐HT2A receptors

doi:10.1002/JLCR.1124

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Synthesis and in vivo evaluation of [O‐methyl‐11C] 2‐(4‐methoxyphenyl)‐N‐(4‐methylbenzyl)‐N‐(1‐methyl‐ piperidin‐4‐yl)acetamide as an imaging probe for 5‐HT2A receptors

Published Oct 30, 2006 · J. Prabhakaran, R. Parsey, V. J. Majo

Journal of Labelled Compounds and Radiopharmaceuticals

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Abstract

2-(4-Methoxyphenyl)-N-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)acetamide (AC90179, 4), a highly potent and selective competitive 5-HT2A antagonist, was labeled by [11C]-methylation of the corresponding desmethyl analogue 5 with [11C]methyl triflate. The precursor molecule 5 for radiolabeling was synthesized from p-tolylmethylamine in three steps with 46% overall yield. [11C]AC90179 was synthesized in 30 min (30 ± 5% yield, EOS) with a specific activity of 4500 ± 500 Ci/mmol and >99% chemical and radiochemical purities. Positron emission tomography studies in anesthetized baboon revealed that [11C]4 Penetrates the blood–brain barrier (BBB) with a rapid influx and efflux of the tracer in all brain regions. Due to lack of tracer retention or specific binding, [11C]4 cannot be used as PET ligand for imaging 5-HT2A receptors. Copyright © 2006 John Wiley & Sons, Ltd.

Non-RCTAnimal Study

Study Snapshot

[O-methyl-11C] 2(4-methoxyphenyl)-N-(4-methylbenzyl)-N-(1-methylpiperidin-4-yl)acetamide (AC90179) shows potential as a PET ligand for imaging 5-HT2A receptors

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Synthesis and in vivo evaluation of [O‐methyl‐11C] 2‐(4‐methoxyphenyl)‐N‐(4‐methylbenzyl)‐N‐(1‐methyl‐ piperidin‐4‐yl)acetamide as an imaging probe for 5‐HT2A receptors

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