The sulfhydryl alkylating reagent N-ethylmaleimide (NEM) blocks opioid receptor binding and receptor/G-protein coupling. Sodium partially restores [ 3 H]naloxone binding after inhibition by NEM to reveal sodium-dependent [ 3 H]naloxone sites, defined as binding in the presence of 50-100 mM NaCl afte
Heterogeneity of sodium-dependent excitatory amino uptake mechanisms in rat brain
β Scribed by Dr. J. Ferkany; J.T. Coyle
- Publisher
- John Wiley and Sons
- Year
- 1986
- Tongue
- English
- Weight
- 828 KB
- Volume
- 16
- Category
- Article
- ISSN
- 0360-4012
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β¦ Synopsis
The pharmacologic and kinetic characteristics of sodium-dependent uptake of 13H]L-glutamate, [3H]D-aspartate, and [3H]L-aspartate into crude synaptosomal preparations of rat corpus striatum and cerebellum have been examined in vitro. In cerebellum the apparent K,s and V, , , for the three excitatory amino acids were identical whereas in striatal synaptosomes, the V, , , for [3H]L-glutamate was 30 % greater (P< .001) than for [3H]D-aspartate and 50% greater (P< .001) than for [3H]L-aspartate. L-Amino adipic acid inhibited the uptake of the three amino acids in both regions of brain but was 15-to 20-fold more potent in cerebellum than in striatum. In contrast, dihydrokainic acid inhibited transport processes in the corpus striatum but was without activity in cerebellar preparations. The neurotoxin kainic acid blocked only a portion (60%) of [3H]L-glutamate and [3H]D-aspartate uptake in cerebellum while completeley inhibiting amino acid transport in corpus striatum. Three days post kainic acid lesion, [3H]D-aspartate uptake was attenuated more than [3H]L-glutamate uptake in the corpus striatum; destruction of corticostriatal afferents reduced [3H]L-glutamate to a greater extent than [3H]D-aspartate. Various lesions of the cerebellum affected excitatory amino acid transport processes to a similar extent. These results suggest that excitatory amino acid transport systems are pharmacologically distinct in different brain regions and may be heterogeneous within a single region.
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