TV-methyl-D-aspartate

Receptors for PCP have been identified in the brain, and PCP acts as an antagonist on the TV-methyl-D-aspartate (NMDA) subtype of glutamate receptors. The drug is unique among hallucinogens in that animals will self-administer it. 

The chemically and radiochemically pure NCA 5-[18F]fluoromethyl- and 5-/ -[18F]fluo-roethyl-10,ll-dihydro-5/7-dibenzo[tf, d]cyclohepten-5, 10-imines 151 and 152 have been prepared for i.v. injection from [18F]fluoride by nucleophilic substitution at the cyclic sulphamates 153 and 154 (equation 96). The labelled products 151 and 152 have been evaluated for receptor binding in animals and in man189. MK801, 155, readily crosses the BBB in mammals and binds to a high affinity site on the TV-methyl-D-aspartate receptor190. 

The cis-156 and trans-151 isomers of FTCP, the fluorine-substituted analogues of the potent TV-methyl-D-aspartate (NMDA) receptor channel blocker l-[l-(2-thienyl)cyclo-hexyl]piperidine (possessing the anticonvulsant action and possible protection from ischemic brain damage191), have been fluorine-18 labelled192 (equation 97). 

Increased production of metabolites of phenylalanine that inhibit synthesis of a variety of substances required for normal brain growth Inhibition of TV-methyl-D-aspartate receptors, which are involved in memory and learning Competitive inhibition of transport of other amino acids required for protein synthesis Impaired polyribosome formation or stabilization Reduced synthesis/increased degradation of myelin Decreased formation of norepinephrine and serotonin Altered myelin structure and function... 

Blank T, Nijholt I, Teichert U, Kugler H, Behrsing H, Fienberg A, Greengard P, Spiess J (1997) The phosphoprotein DARPP-32 mediates cAMP-dependent potentiation of striatal TV-methyl-D-aspartate responses. Proc Natl Acad Sci USA 94 14859-14864. 

MSG is commercially (and even at homes) added to many foods as a flavor enhancer despite the fact that it is an excitatory neurotoxin that can freely penetrate certain brain regions and rapidly destroy neurons by hyperactivating TV-methyl-D-aspartate (NMDA) receptors, a property of MSG that makes the nervous systems of developing fetus particularly vulnerable to this excitotoxinJ39 ... 

Monnet, F.P., Debonnel, G., Fournier, A. deMontigny, C. (1992b) Neuropeptide Y potentiates the TV-methyl-D-aspartate response in the CA3 dorsal hippocampus, involvement of a subtype of sigma receptor. J. Pharmacol. Exp. Ther. 263, 1219-1225. 

TV -Methyl-D-aspartic acid receptor NR2D subunuit Proline-rich fragment 208... 

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