𝔖 Bobbio Scriptorium
✦   LIBER   ✦

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

✍ Scribed by Jaya Prabhakaran; Ramin V. Parsey; Vattoly J. Majo; Ronald L. Van Heertum; J. John Mann; J. S. Dileep Kumar

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
224 KB
Volume
49
Category
Article
ISSN
0022-2135

No coin nor oath required. For personal study only.

✦ Synopsis

Abstract

2‐(4‐Methoxyphenyl)‐N‐(4‐methylbenzyl)‐N‐(1‐methylpiperidin‐4‐yl)acetamide (AC90179, 4), a highly potent and selective competitive 5‐HT~2A~ antagonist, was labeled by [^11^C]‐methylation of the corresponding desmethyl analogue 5 with [^11^C]methyl triflate. The precursor molecule 5 for radiolabeling was synthesized from p‐tolylmethylamine in three steps with 46% overall yield. [^11^C]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 [^11^C]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, [^11^C]4 cannot be used as PET ligand for imaging 5‐HT~2A~ receptors. Copyright © 2006 John Wiley & Sons, Ltd.

📜 SIMILAR VOLUMES

Synthesis of 1-(2,4-dichlorophenyl)-4-cy
Synthesis of 1-(2,4-dichlorophenyl)-4-cyano-5-(4-[11C]methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide ([11C]JHU75528) and 1-(2-bromophenyl)-4-cyano-5-(4-[11C]methoxyphenyl)-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide ([11C]JHU75575) as potential radioligands for PET imaging of cerebral cannabinoid receptor
✍ Hong Fan; Hayden T. Ravert; Daniel P. Holt; Robert F. Dannals; Andrew G. Horti 📂 Article 📅 2006 🏛 John Wiley and Sons 🌐 French ⚖ 183 KB

## Abstract Two novel ligands for cerebral cannabinoid receptor (CB1), 1‐(2,4‐dichlorophenyl)‐4‐cyano‐5‐(4‐methoxyphenyl)‐__N__‐(piperidin‐1‐yl)‐1__H__‐pyrazole‐3‐carboxamide (JHU75528) and 1‐(2‐bromophenyl)‐4‐cyano‐5‐(4‐methoxyphenyl)‐__N__‐(piperidin‐1‐yl)‐1__H__‐pyrazole‐3‐carboxamide (JHU75575)

Synthesis and evaluation of [O-methyl-11
Synthesis and evaluation of [O-methyl-11C]4-[3-[4-(2-methoxyphenyl)- piperazin-1-yl]propoxy]-4-aza-tricyclo[5.2.1.02,6]dec-8-ene-3,5-dione as a 5-HT1A receptor agonist PET ligand
✍ Vattoly J. Majo; Ramin V. Parsey; Jaya Prabhakaran; J. John Mann; J. S. Dileep K 📂 Article 📅 2008 🏛 John Wiley and Sons 🌐 French ⚖ 189 KB 👁 1 views

## Abstract 4‐[3‐[4‐(2‐Methoxyphenyl)piperazin‐1‐yl]propoxy]‐4‐aza‐tricyclo[5.2.1.02,6]dec‐8‐ene‐3,5‐dione (4), a potent and selective 5‐HT~1A~ agonist, was labeled by ^11^C‐methylation of the corresponding desmethyl analogue 3 with ^11^C‐methyl triflate. The precursor molecule 3 was synthesized fr

6-[123I]Iodo-2-[[4-(2-methoxyphenyl) pip
6-[123I]Iodo-2-[[4-(2-methoxyphenyl) piperazin-1-yl]methyl]imidazo[1,2-a]pyridine as potential SPECT agent for imaging dopamine D4 receptor: synthesis and in vivo evaluation in a nonhuman primate
✍ David Alagille; Andrei O. Koren; Greg Kudej; Julie Staley; Kelly Cosgrove; John 📂 Article 📅 2008 🏛 John Wiley and Sons 🌐 French ⚖ 129 KB 👁 1 views

## Abstract The dopamine D~4~ receptor subtype has drawn considerable attention due to its potential implication in schizophrenia and erectile dysfunction. 6‐[^123^I]Iodo‐2‐[[4‐(2‐methoxyphenyl)piperazin‐1‐yl]methyl]imidazo[1,2‐__a__]pyridine [^123^I]‐1, a potent and selective new dopamine D~4~ ago

Radiosynthesis of 2-[6-chloro-2-(4-iodop
Radiosynthesis of 2-[6-chloro-2-(4-iodophenyl)imidazo[1,2-a]pyridin-3-yl]-N-ethyl-N-[11C]methyl-acetamide, [11C]CLINME, a novel radioligand for imaging the peripheral benzodiazepine receptors with PET
✍ C. Thominiaux; F. Mattner; I. Greguric; H. Boutin; F. Chauveau; B. Kuhnast; M.-C 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 French ⚖ 145 KB

## Abstract Recently, a new 2‐(iodophenyl)imidazo[1,2‐__a__]pyridineacetamide series has been developed as iodine‐123‐labelled radioligands for imaging the peripheral benzodiazepine receptors using single photon emission tomography. Within this series, 2‐[6‐chloro‐2‐(4‐iodophenyl)‐imidazo[1,2‐__a__