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Synthesis and 124I-labeling of m-iodophenylpyrrolomorphinan as a potential PET imaging agent for delta opioid (DOP) receptors

✍ Scribed by Eyup Akgün; Philip S. Portoghese; Munawwar Sajjad; Hani A. Nabi

Publisher
John Wiley and Sons
Year
2007
Tongue
French
Weight
119 KB
Volume
50
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Condensation of phenylazo‐β‐ketoamide 4 with oxymorphone 5 afforded an m‐iodophenylpyrrolomorphinan (m‐IPPM) 6 mediated by elemental zinc in acetic acid/sodium acetate buffer. m‐IPPM 6 is a novel opioid receptor agonist (K~i~ = 4.53 nM for DOP) with high selectivity for DOP receptors. m‐IPPM 6 was converted into the positron emitter m‐[^124^I]PPM 8 via the stannylated intermediate 7. The final yield was 24.5 ± 1.9 % (n = 6) with a specific activity of 2.5 ± 1.2 Ci/µmol. Copyright © 2007 John Wiley & Sons, Ltd.

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