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Glycine-related amino acids stereoselectively affect N-methyl-d-aspartate receptor-mediated contractions of guinea pig ileum: Comparison with the inhibition of strychnine-insensitive [3H]glycine binding to rat cortical membranes
| Content Provider | Semantic Scholar |
|---|---|
| Author | Galli, A. Franchi-Micheli, Sergio Mori, Fuminobu Luzzi, S. Zilletti, Lucilla |
| Copyright Year | 1990 |
| Abstract | Ten microM glycine, D-serine and D-alanine potentiated L-glutamate (30 microM)-induced contractions of the guinea pig ileum by an average of 35, 53 and 24%, respectively. On the contrary, D-cysteine, at the same concentration, caused a 21% inhibition of the contractile response to L-glutamate. This inhibitory effect of D-cysteine was abolished by 10 microM glycine. The corresponding L-isomers of these amino acids, namely L-serine, L-alanine and L-cysteine and the other amino acids tested, possessed negligible activity or were inactive in this test. The IC50 values of the same compounds for strychnine-insensitive binding of [3H]glycine (20 nM) to cortical membranes from the brain of the rat were: 0.26 microM, glycine; 1.2 microM, D-serine; 2.1 microM, D-alanine; 8.6 microM, D-cysteine; 51 microM, L-serine; 90 microM, L-alanine; greater than 1000 microM, L-cysteine. On the whole, these results point out a strict requirement for stereoselectivity for both of the effects examined. In addition, the results obtained in the ileum preparation suggest that D-cysteine may act as an antagonist, rather than as an agonist at the glycine site which regulates the responses of N-methyl-D-aspartate receptors. |
| Starting Page | 145 |
| Ending Page | 150 |
| Page Count | 6 |
| File Format | PDF HTM / HTML |
| DOI | 10.1016/0028-3908(90)90054-U |
| PubMed reference number | 2158634 |
| Journal | Medline |
| Volume Number | 29 |
| Alternate Webpage(s) | https://api.elsevier.com/content/article/pii/002839089090054U |
| Alternate Webpage(s) | https://www.sciencedirect.com/science/article/pii/002839089090054U?dgcid=api_sd_search-api-endpoint |
| Alternate Webpage(s) | https://doi.org/10.1016/0028-3908%2890%2990054-U |
| Journal | Neuropharmacology |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |