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Synthesis, radio-LC-MS analysis and biological evaluation of 99mTc-techmazenil

✍ Scribed by Davy Kieffer; Bernard Cleynhens; Kristin Verbeke; Hubert Vanbilloen; Tjibbe de Groot; Christelle Terwinghe; Alfons Verbruggen; Guy Bormans

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
137 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A ^99m^Tc‐labelled compound with the biological characteristics of flumazenil would be useful for determination of neuronal viability after the onset of a stroke. Therefore, we have derivatized Ro‐15‐3890 (a flumazenil metabolite bearing a carboxylic acid group instead of an ethyl ester) by coupling it with a bisamino bisthiol tetraligand bearing a 3‐hydroxypropyl side chain (3‐hydroxypropyl‐BAT) to enable labelling with technetium‐99m. After purification by RP‐HPLC, the ligand was deprotected and labelled in a ‘one pot’ reaction, yielding a ^99m^Tc‐BAT‐propylester of Ro‐15‐3890 (^99m^Tc‐techmazenil). Radio‐LC‐MS analysis of the isolated main peak showed the molecular ion mass (608.0618) of the expected ^99m^Tc‐techmazenil. The biodistribution of ^99m^Tc‐techmazenil was investigated in normal mice and indicated that the tracer is cleared from plasma mainly by the hepatobiliary system and shows a very low uptake in brain. In vitro binding studies on mice brain slices indicated that techmazenil does not bind to benzodiazepine receptors. Copyright © 2004 John Wiley & Sons, Ltd.

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