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Synthesis of [18F]phencyclidines for glutamate receptor mapping

✍ Scribed by M.E. Van Dort; D.J. Yang; M.R. Kilbourn; D.J. Gole; A. Kalir; E.F. Domino; A.B. Young; D.M. Wieland

Publisher
John Wiley and Sons
Year
1989
Tongue
French
Weight
87 KB
Volume
26
Category
Article
ISSN
0022-2135

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✦ Synopsis

L-Glutamate is a major excitatory neurotransmitter in the mammalian brain. Excessive stimulation of excitatory amino acid receptors has been implicated in neurodegenerative disorders such as Alzheimers disease (1); hypofunction of the glutamate system may be involved in schizophrenic-like disorders (2). Three distinct pharmacological classes of glutamate receptors have been identified which reflect the actions of the relatively selective agonists kainate, quisqualate and N-methyl-D-aspartate (NMDA).

Recent findings (3) suggest that drugs such as phencyclidine (PCP) and the PCP analog TCP bind either to an allosteric NMDA site or possibly t o the open channel itself. These findings have created a renewed interest developing a radiolabeled PCP-like compound for mapping NMDA-linked glutamate receptors in the mammalian brain by PET.

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