The 5-(P--fluoro)ethyl analogue 1 of MK 801 2 was synthesized and labelled with 18F in order to visualize the NMDA receptors by positron emission tomography. A tosyloxy precursor 3 was synthesized in 8 steps from dibromodibenzosuberone; the nucleophilic substitution of the tosyl group of 2 by the K
Synthesis of [18F] analogues of MK-801
β Scribed by A. Denis; C. Crouzel
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 73 KB
- Volume
- 26
- Category
- Article
- ISSN
- 0022-2135
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β¦ Synopsis
The major excitatory amino acids in mammalian CNS. L. glutamate and L. aspartate, have neurotoxic activity mediated through excitatory synaptic receptors such as N-methyl-Daspartate (N.M.D.A) receptor subtype.These excitotoxics amino acids have been implicated in several brain damages associated with epilepsy. anoxia-ischemia and hypoglycemia (1).
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Aromatic Analogues of Arcaine Inhibit MK-801 Binding to the NMDA Receptor. -A novel series of analogues such as (VII) and (IX) are synthesized. The most active compound is a derivative of (IX) without the methoxy substituent. The structure-activity relationships are discussed.