Brief Presentation of the Story and Present Status of Studies of the Vertebrate Cholinergic System

Karczmar, Alexander G.

doi:10.1038/npp.1993.81

Cited by 43 publications

(19 citation statements)

References 89 publications

(124 reference statements)

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“…The NIR-spontaneous locomotor behaviour phenomenon is regulated by multiple neurotransmitter systems (Karczmar, 1993). Such transmitters include acetylcholine (ACh), dopamine, serotonin (5-HT), gamma-amino butyric acid (GABA), opioid and noradrenaline (Garrett et al, 2003;Jordan, 1998;Karczmar 1993). This study was able to establish that the inhibitory activity of the extract and the butanol fractions of the plant on NIR and spontaneous locomotor activity (SLA) were mediated via the GABA and (to a lesser extent) opioid receptors.…”

Section: Discussionmentioning

confidence: 99%

Sedative and anxiolytic effects of the extracts of the leaves of <i>Stachytarpheta Cayennensis</i> in mice

Olayiwola

Ukponmwan²,

Olawode³

2013

Afr. J. Trad. Compl. Alt. Med.

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The leaves are used ethnomedicinally in Nigeria and other parts of the world for insomnia and anxiety among other uses. The investigations sought scientific evidence for the ethnomedicinal use of the leaves for the management of insomnia and anxiety as well as the neural mechanisms for the activities. The sedative and anxiolytic effects of the extracts of the leaves of Stachytarpheta cayennensis were examined in this study. The methanolic extract (5-50 mg/kg, i.p.) as well as the ethylacetate (10-50 mg/kg, i.p.), butanol and aqueous fractions (5-50 mg/kg, i.p.) of the extract were examined. Sedation was assessed as reduced novelty-induced rearing (NIR), reduced spontaneous locomotor activity (SLA) and increased pentobarbitone-induced sleeping time (PIST) in mice. The anti-anxiety effect (methanol 2.5-5.0; butanol 5.0; aqueous 20.0; ethylacetate 25.0 mg/kg, i.p.) was assessed using an elevated plus maze. LD 50 was calculated for the extract and the fractions after the intraperitoneal route of administration using the Locke method. The methanolic extract, the butanol and the aqueous fractions inhibited rearing and spontaneous locomotion but prolonged pentobarbitone induced sleep. The ethylacetate fraction however increased both rearing and locomotion and decreased pentobarbitone sleeping time. The butanol and aqueous fractions, but not the methanol extract showed indices of open arm avoidance consistent with anti-anxiety effect. Naltrexone (2.5 mg/kg, i.p.) reversed the inhibition of rearing, locomotion and prolongation of pentobarbitone sleep due to the aqueous fraction of the extract. Flumazenil (2mg/kg, i.p.) abolished the effects of both methanolic extract and the butanol fraction on rearing, locomotion, pentobarbitone sleep and anxiety model. The methanolic extract, the butanol and aqueous fractions possess sedative activity while the ethylacetate fraction possesses stimulant property. The anxiolytic effect was found in both the aqueous fraction and the butanol fraction but not in the main methanol extract and also not in the ethylacetate fraction. Flumazenil, blocked the effect of the leaves of Stachytarpheta cayennensis on rearing, locomotion and elevated plus maze suggesting that GABA receptors are involved in the observed sedative and anxiolytic activities. This study also found opioid receptors involved in the sedative activity of the leaves of Stachytarpheta cayennensis. The rationale for the ethnomedicinal use of the leaves for the management of insomnia and anxiety were confirmed scientifically in this study.

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Section: Discussionmentioning

confidence: 99%

Sedative and anxiolytic effects of the extracts of the leaves of <i>Stachytarpheta Cayennensis</i> in mice

Olayiwola

Ukponmwan²,

Olawode³

2013

Afr. J. Trad. Compl. Alt. Med.

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“…ACh was the first neurotransmitter to be reported (Loewi, 1921) and has since been shown to play a pivotal role in fundamental brain processes such as learning, memory, and sleep (Aigner and Mishkin, 1986;Bartus et al, 1982;Karczmar, 1993). ACh functions in the cholinergic neurons of the peripheral and central nervous systems.…”

Section: Introductionmentioning

confidence: 99%

Structural insights and functional implications of choline acetyltransferase

Govindasamy

Pedersen

Lian

et al. 2004

Journal of Structural Biology

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“…Considering the presence of motor, memory and behavior control circuits in the frontal cortex (Karczmar, 1990, 1993; Pepeu, 1993), we speculate that these are acetylcholinergic circuits and need ChAT to recycle choline in order to maintain the chemical signal to the circuit.…”

Section: Discussionmentioning

confidence: 99%

Neural restrictive silencer factor and choline acetyltransferase expression in cerebral tissue of Alzheimer's Disease patients: a pilot study

et al. 2013

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Decreased Choline Acetyltransferase (ChAT) brain level is one of the main biochemical disorders in Alzheimer’s Disease (AD). In rodents, recent data show that the CHAT gene can be regulated by a neural restrictive silencer factor (NRSF). The aim of the present work was to evaluate the gene and protein expression of CHAT and NRSF in frontal, temporal, entorhinal and parietal cortices of AD patient brains. Four brains from patients with AD and four brains from subjects without dementia were studied. Cerebral tissues were obtained and processed by the guanidine isothiocyanate method for RNA extraction. CHAT and NRSF gene and protein expression were determined by reverse transcription-polymerase chain reaction (RT-PCR) and Western blotting. CHAT gene expression levels were 39% lower in AD patients as compared to the control group (p < 0.05, U test). ChAT protein levels were reduced by 17% (p = 0.02, U test). NRSF gene expression levels were 86% higher in the AD group (p = 0.001, U test) as compared to the control group. In the AD subjects, the NRSF protein levels were 57% higher (p > 0.05, U test) than in the control subjects. These findings suggest for the first time that in the brain of AD patients high NRSF protein levels are related to low CHAT gene expression levels.

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Brief Presentation of the Story and Present Status of Studies of the Vertebrate Cholinergic System

Cited by 43 publications

References 89 publications

Sedative and anxiolytic effects of the extracts of the leaves of <i>Stachytarpheta Cayennensis</i> in mice

Sedative and anxiolytic effects of the extracts of the leaves of <i>Stachytarpheta Cayennensis</i> in mice

Structural insights and functional implications of choline acetyltransferase

Neural restrictive silencer factor and choline acetyltransferase expression in cerebral tissue of Alzheimer's Disease patients: a pilot study

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