Brain regional acetylcholinesterase activity and muscarinic acetylcholine receptors in rats after repeated administration of cholinesterase inhibitors and its withdrawal

Kobayashi, Haruo; Suzuki, Tadahiko; Sakamoto, Maki; Hashimoto, Wataru; Kashiwada, Keiko; Sato, Itaru; Akahori, Fumiaki; Satoh, Tetsuo

doi:10.1016/j.taap.2006.11.006

Cited by 17 publications

(22 citation statements)

References 33 publications

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“…Functional imbalance in neurotransmitter systems triggers adaptive mechanisms. The well known adaptation to OP intoxication consists in down-regulation of cholinergic receptors [8,9]. Another one is the activation of AChE synthesis [10,11].…”

Section: Animalsmentioning

confidence: 99%

Partial protection from organophosphate-induced cholinesterase inhibition by metyrapone treatment

Świercz

Lutz

Gralewicz

et al. 2013

International Journal of Occupational Medicine and Environmental Health

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Background: Organophosphates are cholinesterase (ChE) inhibitors with worldwide use as insecticides. Stress response, evidenced by a dramatic and relatively long-lasting (several hours) rise in the plasma glucocorticoid concentration is an integral element of the organophosphate (OP) poisoning symptomatology. In rodents, corticosterone (CORT) is the main glucocorticoid. There are several reports suggesting a relationship between the stressor-induced rise in CORT concentration (the CORT response) and the activity of the cerebral and peripheral ChE. Thus, it seems reasonable to presume that, in OP intoxication, the rise in plasma CORT concentration may somehow affect the magnitude of the OP-induced ChE inhibition. Metyrapone (MET) [2-methyl-1,2-di(pyridin-3-yl)propan-1-one] blocks CORT synthesis by inhibiting steroid 11β-hydroxylase, thereby preventing the CORT response. Chlorfenvinphos (CVP) [2-chloro-1-(2,4-dichlorophenyl) ethenyl diethyl phosphate] is an organophosphate insecticide still in use in some countries. Material and Methods: The purpose of the present work was to compare the CVP-induced effects -the rise of the plasma CORT concentration and the reduction in ChE activity -in MET-treated and MET-untreated rats. Chlorfenvinphos was administered once at 0.0, 0.5, 1.0 and 3.0 mg/kg i.p. Metyrapone, at 100 mg/kg i.p., was administered five times, at 24-h intervals. The first MET dose was given two hours before CVP. Conclusion: The following was observed in the MET-treated rats: i) no rise in plasma CORT concentration after the CVP administration, ii) a reduced inhibition and a faster restitution of blood and brain ChE activities. The results suggest that MET treatment may confer significant protection against at least some effects of OP poisoning. The likely mechanism of the protective MET action has been discussed.

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Section: Animalsmentioning

confidence: 99%

Partial protection from organophosphate-induced cholinesterase inhibition by metyrapone treatment

Świercz

Lutz

Gralewicz

et al. 2013

International Journal of Occupational Medicine and Environmental Health

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“…Relatively little attention has been given to the effects of low-level organophosphate exposure that is not associated with acute cholinergic symptoms (Ray and Richards, 2001). There are only a few reports focused on persistent effects of repeated and low-level exposures to organophosphates on brain regional AChE activity and other neurochemical and behavioral parameters 1.3 EFFECTS OF ORGANOPHOSPHATES AND CARBAMATES ON ACETYLCHOLINESTERASE (Karanth et al, 2007;Kobayashi et al, 2007;Ma et al, 2001;Sun et al, 2003;Terry et al, 2007). Terry et al (2007) injected rats with chlorpyrifos at doses of 2.5, 10.0, and 18.0 mg/kg, subcutaneously (s.c.) every other day over the course of 30 days and then gave a twoweek washout period.…”

Section: Effects Of Organophosphates On Regional Brain Acetylcholinesmentioning

confidence: 99%

“…In another study, Kobayashi et al (2007) measured AChE activity in the striatum, hippocampus, and cerebral cortex of rats after they were treated with dichlorvos (DDVP) at 3 mg/ kg/day, s.c., for 7 and 14 days. AChE activity was assayed 1, 6, and 11 days after the last treatment with DDVP (Kobayashi et al, 2007).…”

Section: Effects Of Organophosphates On Regional Brain Acetylcholinesmentioning

confidence: 99%

“…AChE activity was assayed 1, 6, and 11 days after the last treatment with DDVP (Kobayashi et al, 2007). AChE activity was markedly decreased in the three brain regions 1 day after treatment over both 7 and 14 days.…”

Section: Effects Of Organophosphates On Regional Brain Acetylcholinesmentioning

confidence: 99%

“…Asterisks indicate values that are significantly different from control value ( Ã p , 0.05, ÃÃÃ P , 0.01). Adapted from Kobayashi et al (2007).…”

Section: Effects Of Carbamates On Brain Regional Acetylcholinesterasementioning

confidence: 99%

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Acetylcholinesterase and Acetylcholine Receptors: Brain Regional Heterogeneity

Kobayashi

Suzuki

Akahori

et al. 2011

Anticholinesterase Pesticides

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Simple validated method of LC–MS/MS determination of BZ agent in rat plasma samples

Herman

Dlabková

Cechova

et al. 2020

Drug Testing and Analysis

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Agent BZ (3‐quinuclidinyl benzilate) is a centrally acting synthetic anticholinergic agent, considered as a potential military incapacitating chemical warfare agent. Despite its significance as a model compound in pharmacological research and its potential misuse in chemical attacks, few modern analytical methods for BZ determination in biological samples have been published. The goal of the present work is to develop and validate a sensitive and rapid LC–MS/MS method for the determination of agent BZ in rat plasma. The sample preparation was based on solid‐phase extraction on C‐18 cartridges. The reversed‐phase HPLC coupled with the mass spectrometer with electrospray ionization in the positive ion‐selective reaction monitoring mode was employed in the BZ analysis. Atropine was used as an internal standard. The presented method is selective, accurate, precise, and linear (r2 = 0.9947) in a concentration range from 0.5 ng/mL to 1 000 ng/mL and sensitive enough (limit of detection 0.2 ng/mL; limit of quantification 0.5 ng/mL) to determine the BZ plasma levels in rats exposed to 2 mg/kg and 10 mg/kg of BZ. The highest level of BZ in plasma was observed 5 minutes after intramuscular administration (154.6 ± 22.3 ng/mL in rats exposed to 2 mg/kg of BZ and 1024 ± 269 ng/mL in rats exposed to 10 mg/kg). After 48 h, no BZ was observed at detectable levels. This new method allows the detection and quantification of BZ in biological samples after exposure of an observed organism and it will be further optimized for other tissues to observe the distribution of BZ in organs.

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Brain regional acetylcholinesterase activity and muscarinic acetylcholine receptors in rats after repeated administration of cholinesterase inhibitors and its withdrawal

Cited by 17 publications

References 33 publications

Partial protection from organophosphate-induced cholinesterase inhibition by metyrapone treatment

Partial protection from organophosphate-induced cholinesterase inhibition by metyrapone treatment

Acetylcholinesterase and Acetylcholine Receptors: Brain Regional Heterogeneity

Simple validated method of LC–MS/MS determination of BZ agent in rat plasma samples

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