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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

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

Publisher
John Wiley and Sons
Year
2008
Tongue
French
Weight
189 KB
Volume
51
Category
Article
ISSN
0022-2135

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✦ Synopsis

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 from commercially available endo‐N‐hydroxy‐5‐norbornene‐2,3‐dicarboximide in two steps with an overall yield of 40%. Radiosynthesis of ^11^C‐4 was achieved in 35 min in 20±5% yield (n=6) at the end of synthesis with a specific activity of 2600±250 Ci/mmol. In vivo positron emission tomography (PET) studies in baboon revealed rapid uptake of the tracer into the brain. However, lack of specific binding indicates that ^11^C‐4 is not useful as a 5‐HT~1A~ agonist PET ligand for clinical studies. Copyright © 2008 John Wiley & Sons, Ltd.

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