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Synthesis and evaluation of new 18F-labelled thienylcyclohexylpiperidine (TCP) analogues as radioligands for the NMDA receptor-channel complex

✍ Scribed by Yoshihiko Shibayama; Shigeki Sasaki; Urara Tomita; Toru Nishikawa; Minoru Maeda

Publisher
John Wiley and Sons
Year
1996
Tongue
French
Weight
729 KB
Volume
38
Category
Article
ISSN
0022-2135

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✦ Synopsis

We have synthesized new fluorine-18 labelled derivatives of thienylcyclohexylpiperidine (TCP), a non-competitive antagonist of NMDA receptor, which binds to the phencyclidine (PCP) binding site located within the receptor-associated ion channel. The mesylate precursors for (1S* ,Z*)-2-(hydroxymethyl)-and (lS*,2R*)-2-(methoxymethyoxymethyl)-1 -(N-piperidyl)-1 -[2-(2'4' 8FJfluoroethyl) thiophenyl]cyclohexane, ['*F]4 and ["FJ19, respectively, were prepared from 2-hydroxycyclo-hexanone. Radiochemical syntheses were done by displacement of the mesylates by ['8F]fluoride ion with nocarrier-added [W2.2.2]+'*F in 4-4.5 % radiochemical yields with specific activity of >31 GBqlmol. In the biodistribution studies with ["F]4 and [18F]1 9, no selective accumulation of radioactivity was observed. Low affinities of these ligands to the NMDA receptor were also shown in in vitro binding experiments.

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