Effects of E2020 on the extracellular levei of acetylcholine in the rat cerebral cortex measured by microdialysis without addition of cholinesterase inhibitor

Kosasa, Takashi; Yamanishi, Yukinori; Ogura, Hiroo; Yamatsu, Kiyomi

doi:10.1016/0014-2999(90)92282-n

Cited by 14 publications

(7 citation statements)

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“…AF102B, a M1 muscarinic receptor agonist, increases the ACh levels in dialysates from the hippocampus (Ogane etal., 1990), and the acetylcholinesterase inhibitors, tetrahydroaminoacridine and E2020, also increase ACh in the rat cerebral cortex (Kosaka et al, 1990). All three compounds have ameliorative effects on drug-induced amnesia, but, unlike them, nefiracetam is not a ligand for muscarinic receptors, because it does not displace the binding of quinuclidinylbenzilate (Nabeshima et al, 1991).…”

Section: Discussionmentioning

confidence: 97%

Nefiracetam enhances acetylcholine outflow from the frontal cortex: in vivo microdialysis study in the rat

Kawajiri¹,

Taniguchi²,

Sakurai³

et al. 1994

J. Neural Transmission

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The effects of nefiracetam [DM-9384; N-(2, 6-dimethylphenyl)-2-(2-oxo-1-pyrrolidinyl)acetamide], a cognitive enhancer, on extracellular acetylcholine and glutamic acid in the frontal cortex were studied using brain microdialysis in freely moving rats. Nefiracetam administration (1 mg/kg, p.o.) doubled the amount of acetylcholine in the dialysate. When tetrodotoxin was added to the perfusion solution, the basal level of acetylcholine decreased and nefiracetam caused no increase in acetylcholine outflow. The amount of glutamic acid in the dialysates was not affected by nefiracetam. These results suggest that nefiracetam increases the amount of acetylcholine within the cholinergic synaptic clefts.

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Section: Discussionmentioning

confidence: 97%

Nefiracetam enhances acetylcholine outflow from the frontal cortex: in vivo microdialysis study in the rat

Kawajiri¹,

Taniguchi²,

Sakurai³

et al. 1994

J. Neural Transmission

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“…The cerebral cortex, hippocampus, and striatum were dissected, and ACh was extracted and measured using an HPLC technique. The results (Table 2) indicate that oral administration of donepezil caused a dose‐dependent increase in ACh in all three areas of the brain tested. By using a microdialysis technique, the effect of donepezil on the concentration of ACh in the extracellular space of the rat brain cortex was measured 15. A microdialysis probe was implanted into the cerebral cortex of conscious rats and perfused with buffer.…”

Section: Donepezil Hydrochloride (E2020)mentioning

confidence: 99%

“…By using a microdialysis technique, the effect of donepezil on the concentration of ACh in the extracellular space of the rat brain cortex was measured 15. A microdialysis probe was implanted into the cerebral cortex of conscious rats and perfused with buffer.…”

Section: Donepezil Hydrochloride (E2020)mentioning

confidence: 99%

Donepezil hydrochloride: A treatment drug for Alzheimer?s disease

Sugimoto

2001

Chem. Record

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The role of the cholinergic system with respect to cognitive deficits characteristic of Alzheimer's disease (AD) has led to a number of studies focusing on the development of acetylcholinesterase (AChE) inhibitors as a drug for treating this disease. The earliest known AChE inhibitors, namely, physostigmine and tacrine, performed poorly in clinical trials (e.g., poor oral activity, brain penetration, and hepatotoxic liability). Studies were then focused on finding a new type of acetylcholinesterase inhibitor that would overcome the disadvantages of these two compounds. Donepezil hydrochloride inaugurates a new class of AChE inhibitors with longer and more selective action and with manageable adverse effects.

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“…Recently, effects of some drugs on extracellular ACh concentrations have been reported using the microdialysis procedure without the use of ChE inhibitor in the perfu sion fluid (12)(13)(14)(15)(16)(17). However, in those studies, the effects of only i.p.…”

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confidence: 99%

Effect of NIK-247 on Basal Concentrations of Extracellular Acetylcholine in the Cerebral Cortex of Conscious, Freely Moving Rats

Ishii

Kojima

Ikeda

et al. 1994

Japanese Journal of Pharmacology

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ABSTRACT-We studied the effect of orally administered 3,5,6,7,quinoline monohydrochloride monohydrate) on basal extracellular acetylcholine (ACh) con centrations in the rat cerebral cortex using microdialysis without the addition of cholinesterase inhibitor to the perfusion fluid and radioimmunoassay for ACh. In addition, the effect of oral administration of NIK 247 on acetylcholinesterase (AChE) activity in rat cerebral cortex was determined. The mean basal ACh con tent in the perfusate from the cerebral cortex of freely moving rats was 123.2±21.8 fmol/30 min (n=7). NIK-247 (2.5 10.0 mg/kg, p.o.) increased the ACh content of the perfusate in a dose-dependent manner. NIK-247 at 10 mg/kg significantly increased the ACh content in the perfusate from 0.5 to 2.5 hr after administration, and the maximum increase was attained at 1 hr after administration. 9-Amino-1,2,3,4 tetrahydroacridine (5 mg/kg, p.o.) and physostigmine (0.5 mg/kg, i.p.) significantly increased the ACh con tent in the perfusate from 1 to 2 hr and from 0.5 to 1.5 hr after administration, respectively. AChE activities in the cerebral cortex were about 32070 and 1207o below the control value at 1 hr and 3 hr after administration of NIK-247 at 10 mg/kg, respectively. These findings demonstrate that NIK-247 increases extracellular ACh concentration and inhibits AChE activity in the cerebral cortex after oral administration, and they suggest that NIK-247 facilitates central cholinergic transmission.

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Effects of E2020 on the extracellular levei of acetylcholine in the rat cerebral cortex measured by microdialysis without addition of cholinesterase inhibitor

Cited by 14 publications

References 0 publications

Nefiracetam enhances acetylcholine outflow from the frontal cortex: in vivo microdialysis study in the rat

Nefiracetam enhances acetylcholine outflow from the frontal cortex: in vivo microdialysis study in the rat

Donepezil hydrochloride: A treatment drug for Alzheimer?s disease

Effect of NIK-247 on Basal Concentrations of Extracellular Acetylcholine in the Cerebral Cortex of Conscious, Freely Moving Rats

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