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The effect of the selective reversible acetylcholinesterase inhibitor E2020 on extracellular acetylcholine and biogenic amine levels in rat cortex

Giacobini, E ; Zhu X, D ; Williams, E ; Sherman, K A

Neuropharmacology, February 1996, Vol.35(2), pp.205-11 [Tạp chí có phản biện]

ISSN: 0028-3908 ; PMID: 8734490 Version:1

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  • Nhan đề:
    The effect of the selective reversible acetylcholinesterase inhibitor E2020 on extracellular acetylcholine and biogenic amine levels in rat cortex
  • Tác giả: Giacobini, E ; Zhu X, D ; Williams, E ; Sherman, K A
  • Chủ đề: Acetylcholine -- Analysis ; Acetylcholinesterase -- Metabolism ; Biogenic Monoamines -- Analysis ; Cerebral Cortex -- Drug Effects ; Cholinesterase Inhibitors -- Pharmacology ; Indans -- Pharmacology ; Piperidines -- Pharmacology
  • Là 1 phần của: Neuropharmacology, February 1996, Vol.35(2), pp.205-11
  • Mô tả: E2020 is a piperidine cholinesterase inhibitor (ChEI) which is structurally distinct from other compounds presently under study for treatment of Alzheimer's disease. We studied the effect of this compound on acetylcholine (ACh), norepinephrine (NE), dopamine (DA) and serotonin (5-HT; 5-hydroxytryptamine) by means of transcortical microdialysis in the cortex of awake rats with no ChEI in the probe. We also compared the inhibition of brain cholinesterase (ChE) by two different approaches. Following 0.5 and 2.0 mg/kg s.c. administration, the increase in ACh was 200% (30 min) and 2100% (1 hr), respectively. The maximal ChE inhibition at 30 min was 35.5% (2.0 mg/kg) and 15.6% (0.5 mg/kg) when measured as ACh hydrolysis in the diluted homogenate. After the 2.0 mg/kg dose, phosphorylation by DFP was completely blocked at 30 min. After 0.5 mg/kg, ChE phosphorylation was maximally inhibited at 30 min (56%) and declined thereafter to negligible levels by 3 hr. In addition, E2020 increased extracellular...
  • Ngôn ngữ: English
  • Số nhận dạng: ISSN: 0028-3908 ; PMID: 8734490 Version:1

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