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INHIBITION OF GABA UPTAKE IN RAT BRAIN SLICES BY NIPECOTIC ACID, VARIOUS ISOXAZOLES AND RELATED COMPOUNDS
Abstract
—A variety of isoxazoles structurally related to muscimol (3‐hydroxy‐5‐aminomethylisoxazole) were tested as inhibitors of the uptake of GABA and some other amino acids in rat brain slices, and of the activity of the GABA‐metabolizing enzymes l‐glutamate 1‐carboxylyase and GABA:2‐oxo‐glutarate aminotransferase. A bicyclic derivative, 4,5,6,7‐tetrahydroisoxazolo[4,5‐c]pyridin‐3‐ol, proved to be a more potent inhibitor of GABA uptake than muscimol. Structure‐activity studies on this derivative, which appeared to be a competitive inhibitor of GABA uptake, led to the findings that nipecotic acid (piperidine‐3‐carboxylic acid) is a powerful non‐competitive inhibitor of GABA uptake, and that perhydro‐1,2‐oxazine‐6‐carboxylic acid is a relatively weak competitive inhibitor of GABA uptake.
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Citations
Cited by
Feed‐forward dendritic inhibition in rat hippocampal pyramidal cells studied in vitro
Alger, B. E., & Nicoll, R. A. (1982) · The Journal of Physiology · doi:10.1113/jphysiol.1982.sp014255 · Cited by 527
Transport and Metabolism of Glutamate and Gaba in Neurons and Glial Cells
Schousboe, A. (1981) · International Review of Neurobiology · doi:10.1016/s0074-7742(08)60289-5 · Cited by 440
Involvement of P2X7 receptors in the regulation of neurotransmitter release in the rat hippocampus
Sperlágh, B., Köfalvi, A., Deuchars, J., Atkinson, L., J. Milligan, C., Buckley, N. J., & Vizi, E. S. (2002) · Journal of Neurochemistry · doi:10.1046/j.1471-4159.2002.00920.x · Cited by 264
GABA: homeostatic and pharmacological aspects
Schousboe, A., & Waagepetersen, H. S. (2007) · Progress in Brain Research · doi:10.1016/s0079-6123(06)60002-2 · Cited by 121
gamma-Aminobutyric acid uptake by a bacterial system with neurotransmitter binding characteristics.
Guthrie, G. D., & Nicholson-Guthrie, C. S. (1989) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.86.19.7378 · Cited by 61
Metadata
- Authors
- Krogsgaard‐Larsen, P., & Johnston, G. A. R.
- Venue
- Journal of Neurochemistry
- Publisher
- Wiley
- Published
- 1975-12
- Volume
- 25
- Issue
- 6
- Pages
- 797-802
- ISSN
- 0022-3042 (ISSN-L)
- 1471-4159
- OpenAlex
- W1985637710
- Cited by
- 328
- References
- 0
- FWCI
- 4.84
- Type
- journal article
- Language
- en
- Open access
- closed
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- Krogsgaard‐Larsen, P., & Johnston, G. A. R. (1975). INHIBITION OF GABA UPTAKE IN RAT BRAIN SLICES BY NIPECOTIC ACID, VARIOUS ISOXAZOLES AND RELATED COMPOUNDS. Journal of Neurochemistry. https://doi.org/10.1111/j.1471-4159.1975.tb04410.x
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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