Pharmacological Aspects of the Acetylcholinesterase Inhibitor Galantamine

Ago, Yukio; Koda, Ken; Takuma, Kazuhiro; Matsuda, Takehisa

doi:10.1254/jphs.11r01cr

Cited by 96 publications

(57 citation statements)

References 99 publications

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“…On the other hand, memantine administration results in significant increases in extracellular dopamine, noradrenaline, and their metabolites in the cortical regions and in dopamine reduction in rat hippocampus (17). The influence of galantamine and memantine on the release of dopamine and noradrenaline may contribute to the beneficial effects of their co-administration on the non-cognitive symptoms of dementia that are usually correlated to these neurotransmitters (16).…”

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confidence: 98%

Synergistic Effects of Galantamine and Memantine in Attenuating Scopolamine-Induced Amnesia in Mice

et al. 2012

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Abstract.We investigated a possible drug efficacy enhancement obtained by combining inactive doses of galantamine and memantine in the scopolamine-induced amnesia model in mice. We evaluated the effects of the two drugs, either alone or in combination, using the spontaneous alternation and object recognition tasks. In both tests, combination of low doses of galantamine (0.1 mg/kg, s.c.) and memantine (0.5 mg/kg, i.p.), which were sub-active per se, rescued the memory impairment induced by scopolamine (1 mg/kg, i.p.). The results suggest that combinations of galantamine and memantine might provide a more effective treatment of memory impairments in cognitive disorders than either drug used alone.

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confidence: 98%

Synergistic Effects of Galantamine and Memantine in Attenuating Scopolamine-Induced Amnesia in Mice

et al. 2012

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“…Acoustic startle responses were measured in a startle chamber (SR-LAB ® ; San Diego Instruments, San Diego, CA, USA) as described previously (8). After a background noise of 65 dB had been presented for a 5-min acclimation period, each mouse was exposed to four consecutive blocks with a total of 100 trials over the approximately 30-min test session.…”

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confidence: 99%

The Selective Metabotropic Glutamate 2/3 Receptor Agonist MGS0028 Reverses Isolation Rearing–Induced Abnormal Behaviors in Mice

Ago¹,

Araki²,

Yano³

et al. 2012

J Pharmacol Sci

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Abstract. Isolation-induced abnormal behaviors are useful animal models for assessing potential anti-psychotic drugs. This study examined the effect of MGS0028, a selective metabotropic glutamate 2/3 receptor agonist, on abnormal behaviors such as hyperactivity, aggression, and deficits of prepulse inhibition in isolation-reared mice. MGS0028 attenuated hyperactivity and aggressive behaviors in isolation-reared mice. The agonist also reversed isolation rearing-induced deficits of prepulse inhibition. On the other hand, MGS0028 did not affect locomotor activity and prepulse inhibition in group-reared mice. These results suggest that the metabotropic glutamate 2/3 receptor agonist, MGS0028, is a potential compound for the treatment of psychiatric disorders.

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“…20,21 One of the most widely used anti-cholinesterase drug galantamine is derived from plant sources. 22 Nicotinic and muscarinic receptor-modulating properties of galantamine contribute to the antipsychotic effect and development of cognitive dysfunction. Available drugs which are used to treat Alzheimer's disease are mainly the inhibitors of cholinesterase enzymes.…”

Section: Butyrylcholinesterase (Bche) Inhibitory Activitymentioning

confidence: 99%

Phytochemical Screening and Acetylcholinesterase and Butyrylcholinesterase Inhibitory and Thrombolytic Activities of Grewia abutilifolia Vent. & Juss. Leaf

Rafe¹,

Salam

Hossain³

et al. 2018

Dhaka Univ. J. Pharm. Sci

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Cholinesterase inhibitors offer the possible pathway to fight against various types of neurodegenerative diseases. Grewia abutilifolia is used extensively in traditional and folk medicines mainly to improve intellectual capabilities and memory enhancement purposes which support its possible effects against neurodegenerative disorders. We performed preliminary phytochemical screening to observe the presence of potential phytoconstituents of G. abutilifolia leaf extracts and evaluated acetylcholinesterase and butyrylcholinesterase inhibitory properties to measure its anti-cholinesterase activities. Preliminary phytochemical screening confirmed the presence of saponins, tannins, flavonoids, terpenoids, steroids, carbohydrates, coumarins, alkaloids etc. The petroleum ether (PESF), chloroform (CSF) and aqueous soluble fractions (AQSF) of the crude extract of the plant leaf were screened for bioactivities. The highest inhibition of acetylcholinesterase was exhibited by aqueous soluble fraction (AQSF) with IC50 = 5.73 ± 0.59 μg/ml, while the highest inhibition of butyrylcholinesterase was shown by petroleum ether soluble fraction (PESF) with IC50 = 6.57 ± 1.81 μg/ml in a dose-dependent manner. During assay for thrombolytic activity, the chloroform soluble fraction (CSF) revealed highest activity with 25.75 ± 1.62% clot lysis. These results of the present study suggested the effectiveness of G. abutilifolia against various neurological diseases.

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Pharmacological Aspects of the Acetylcholinesterase Inhibitor Galantamine

Cited by 96 publications

References 99 publications

Synergistic Effects of Galantamine and Memantine in Attenuating Scopolamine-Induced Amnesia in Mice

Synergistic Effects of Galantamine and Memantine in Attenuating Scopolamine-Induced Amnesia in Mice

The Selective Metabotropic Glutamate 2/3 Receptor Agonist MGS0028 Reverses Isolation Rearing–Induced Abnormal Behaviors in Mice

Phytochemical Screening and Acetylcholinesterase and Butyrylcholinesterase Inhibitory and Thrombolytic Activities of Grewia abutilifolia Vent. & Juss. Leaf

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