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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Göthert, M. Schultheiss, R. Fink, K. |
| Description | Author Affiliation: Fink K ( Institute of Pharmacology and Toxicology, University of Bonn, Germany.) |
| Abstract | 1. Human brain cortical slices from patients undergoing neurosurgery for treatment of epilepsy resistant to antiepileptic drugs were used to identify and characterize N-methyl-D-aspartate (NMDA) and non-NMDA receptors mediating stimulation of noradrenaline release. The slices preincubated with [3H]-noradrenaline were superfused with Krebs-Henseleit solution with or without Mg2+ (1.2 mmol l-1) and were stimulated by 2-min exposure to NMDA, kainic acid or (RS)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA). 2. In slices superfused without Mg2+, NMDA induced a concentration-dependent tritium overflow. 3. The NMDA-evoked tritium overflow was almost abolished by tetrodotoxin (TTX), Mg2+ or by omission of Ca2+ from the superfusion fluid. 2-Amino-5-phosphonopentanoic acid (AP5; a competitive NMDA receptor antagonist) or dizocilpine (formerly MK-801; an antagonist at the phencyclidine receptor within the NMDA-gated ion channel) inhibited the NMDA-evoked tritium overflow. The stimulatory effect of NMDA was not significantly enhanced by glycine added to the superfusion fluid but was reduced by 7-chlorokynurenic acid (an antagonist at the glycine site coupled to the NMDA receptor). 4. In slices superfused with solution containing Mg2+, kainic acid or AMPA induced a concentration-dependent tritium overflow which was susceptible to blockade by TTX. 5. The kainic acid-evoked tritium overflow was not affected by DL-(E)-2-amino-4-methyl-5-phosphono-3-pentanoic acid (CGP37849; a competitive NMDA receptor antagonist), but was inhibited by 6-cyano-7-nitroquinoxaline-2,3-dione (CNQX; an antagonist at glutamate receptors of the non-NMDA type). 6. The AMPA-evoked tritium overflow was also inhibited by CNQX.2n |
| ISSN | 00071188 |
| e-ISSN | 14765381 |
| Journal | British Journal of Pharmacology |
| Issue Number | 1 |
| Volume Number | 106 |
| Language | English |
| Publisher | Wiley Online Library(on behalf of The British Pharmacological Society) |
| Publisher Date | 1992-05-01 |
| Publisher Place | Great Britain (UK) |
| Access Restriction | Open |
| Subject Keyword | Cerebral Cortex Metabolism Ibotenic Acid Analogs & Derivatives Kainic Acid Pharmacology N-Methylaspartate Norepinephrine Receptors, N-Methyl-D-Aspartate 2-Amino-5-phosphonovalerate 6-Cyano-7-nitroquinoxaline-2,3-dione Drug Effects Dizocilpine Maleate Dose-Response Relationship, Drug Glycine Kynurenic Acid Magnesium Antagonists & Inhibitors Quinoxalines Tetrodotoxin Tritium Alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmacology |
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