Anticonvulsant drugs and brain glucose

Gilbert, John; Gray, P. P.; Heaton, Gillian M.

doi:10.1016/0006-2952(71)90492-8

Cited by 15 publications

(4 citation statements)

References 8 publications

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“…However, determinations of the sodium contents of slices incubated in the bicarbonate medium showed that, in contrast to the observation of Woodbury, Koch & Vernadakis (1958), acetazolamide (20 gM) did not significantly alter the sodium gradient. Initial velocity studies of xylose uptake indicated that the drug altered both the apparent dissociation constant of the carrier-xylose complex and the maximal transport rate in a manner compatible with previous observations (Gilbert, Gray & Heaton, 1971) and with the inhibition of xylose uptake from a medium containing 1 mm xylose. A high concentration of acetazolamide (200 pM) did not inhibit the active transport of xylose by the tissue but significantly increased the sodium gradient.…”

Section: Qdsupporting

confidence: 57%

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Proceedings of the British Pharmacological Society

1971

British J Pharmacology

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Section: Qdsupporting

confidence: 57%

“…Acetazolamide can influence xylose uptake by the slices (Gilbert, Gray & Heaton, 1971). It has also been reported to increase the sodium gradient (Nao/Nai) in brain (Woodbury, Koch & Vernadakis, 1958).…”

Section: Qdmentioning

confidence: 99%

Proceedings of the British Pharmacological Society

1971

British J Pharmacology

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“…The theory that the increase in the glucose concentration of the brain caused by all the anticonvulsants tested is involved in their action through membrane stabilization (Gilbert, Gray & Heaton, 1971) has received support (Nahorski, 1972) but it is a difficult one to test. Of the other effects of the drugs the changes which some induce in brain sodium, potassium-activated, magnesium-dependent adenosine triphosphatase (Na+,K+-ATPase, EC.3.6.1.3) activity, thereby influencing ion gradients, are of particular interest.…”

Section: Introductionmentioning

confidence: 99%

Effects of Anticonvulsant and Convulsant Drugs on the Atpase Activities of Synaptosomes and Their Components

Gilbert

Wyllie

1976

British J Pharmacology

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The effects of anticonvulsants, and other drugs on the Na+, K+‐adenosine triphosphatase (ATPase) (ouabain‐sensitive) and Mg++‐ATPase activities of synaptosomes and their components have been determined. The Mg++‐ATPase activity of synaptosomes was not affected by the drugs but the Na+, K+‐ATPase activity was inhibited by phenytoin (diphenylhydantoin), ethosuximide and diazepam. Fractions containing mainly membranes, mitochondria or synaptic vesicles, were prepared from synaptosomes by osmotic shock and subsequent density gradient centrifugation. Inhibition of Na+, K+‐ATPase activity by phenytoin, ethosuximide and diazepam was apparent only in the membrane fraction. The fraction containing synaptic vesicles exhibited pronounced Mg++‐ATPase but no Na+, K+‐ATPase activity. In contrast to the enzymes of the membranes and mitochondria, the Mg++‐ATPase of the vesicles was inhibited by diazepam and all of the anticonvulsants tested.

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“…This motif can be found in metabolites from organisms such as fungi, bacteria, plants or even animals. Accordingly, structural features of natural γ‐lactams are also wide and are a great inspiration to develop new biologically active molecules, for example approved drugs such as Doxapram, [16] a respiratory stimulant, Ethosuximide, [17] used to treat absence seizures or Piracetam, [18] useful to improve cognitive powers and memory ( Figure 1).…”

Section: Introductionmentioning

confidence: 99%

γ‐Lactam‐Based Antifungal Compounds against the Wheat Pathogen Zymoseptoria tritici

Damiens

Dascălu²,

Furman

et al. 2021

Chemistry & Biodiversity

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As new environmentally friendly and effective antifungal agents are deeply needed, efficient ecofriendly strategies were designed to access two series of compounds inspired from natural γ‐lactams. Designed compounds were fully characterized and evaluated as antifungal candidates against Zymoseptoria tritici, the main pathogen on wheat crops. The targeted derivatives were prepared from natural resources using green solvents, simple procedures, and limited purification steps. These bio‐inspired compounds revealed as good candidates for further development of efficient crop protection products. Indeed, the HIT compounds exhibited IC50 around 1 μg/mL and were more active than the references tebuconazole and bixafen towards some multidrug‐resistant strains. Two dozen of derivatives have been obtained for each series and allowed to establish early structure‐activity relationships useful for the development of next generation of γ‐lactam derivatives with improved efficacy.

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Anticonvulsant drugs and brain glucose

Cited by 15 publications

References 8 publications

Proceedings of the British Pharmacological Society

Proceedings of the British Pharmacological Society

Effects of Anticonvulsant and Convulsant Drugs on the Atpase Activities of Synaptosomes and Their Components

γ‐Lactam‐Based Antifungal Compounds against the Wheat Pathogen Zymoseptoria tritici

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