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 wit
Happing cation channels: Synthesis of [125I] and [18F] analogs of MK-801
✍ Scribed by D.M. Wieland; M.R. Kilbourn; E. Laborde; D.J. Yang; J-L. Pirat; D.L. Gildersleeve; M.E. Van Dort; B.J. Ciliax; A.B. Young
- Publisher
- John Wiley and Sons
- Year
- 1989
- Tongue
- French
- Weight
- 110 KB
- Volume
- 26
- Category
- Article
- ISSN
- 0022-2135
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## Abstract The ^125^I analog of MK‐0591, 1, has been prepared for use as a radioligand for developing a 5‐lipoxygenase activating protein (FLAP) binding assay. The radiosynthesis involves a two step oxidative iododestannylation‐saponification procedure. A FLAP binding assay has been developed in h
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