Nootropic drugs and brain cholinergic mechanisms

Pepeu, Giancarlo; Spignoli, G.

doi:10.1016/0278-5846(89)90112-7

Cited by 64 publications

(33 citation statements)

References 50 publications

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“…The actions of Rb| are similar to other nootropic agents, such as piracetam, pramiracetam and oxiracetam, in that these drugs have been reported to stimulate late choline uptake; however, these nootropic agents have not been demonstrated to increase the release of ACh [35],…”

Section: Discussionmentioning

confidence: 65%

“…muscarinic, nicotinic agonists) [30], those which increase the turnover of ACh, generally by nonspecific mechanisms (e.g. piracetam, 4-aminopyridine) [31][32][33], or increasing availability of the synthetic precursor, choline, by dietary supplementation [34], These therapeutic ap proaches have proven to be far from satisfac tory. Experiments presented indicate that the mechanism of Rbi action does not involve cholinesterase inhibition or displacement of scopolamine from the muscarinic receptors.…”

Section: Discussionmentioning

confidence: 99%

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Effects of Ginsenoside Rbi on Central Cholinergic Metabolism

Benishin¹,

et al. 1991

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Ginsenosides, the saponins of ginseng, are bioactive ingredients which exert many beneficial effects. One ginsenoside, Rb₁, extracted from North American ginseng (Panax quinquefolium L.), partially prevents the memory deficits induced by a cholinergic agent (scopolamine) in rats. In vitro studies show that Rb₁ has no effect on quinuclidinyl benzylate binding or on acetylcholinesterase activity, but facilitates the release of acetylcholine (ACh) from hippocampal slices. The increase in ACh release is associated with an increased uptake of choline into nerve endings; however, calcium influx is unaltered. The ability of Rb₁ to prevent memory deficits may be related to facilitation of ACh metabolism in the central nervous system.

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Section: Discussionmentioning

confidence: 65%

Section: Discussionmentioning

confidence: 99%

Effects of Ginsenoside Rbi on Central Cholinergic Metabolism

Benishin¹,

et al. 1991

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“…cholinergic system (Bourson et al 1995;Bourson et al 1998). Furthermore, aniracetam has been shown to modulate cholinergic systems (Bartolini et al 1992;Pepeu and Spignoli 1989). It is tempting to speculate that cholinergic, serotonergic, and glutamatergic systems intersect in the striatum, and the present data reflect a disruption in the way these systems interact.…”

Section: Densensitization Modulatorsmentioning

confidence: 58%

Ionotropic Glutamate Receptor Modulation of 5-HT6 and 5-HT7 mRNA Expression in Rat Brain

Healy

Meador‐Woodruff

1999

Neuropsychopharmacology

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“…Therefore, the potentiation of the cholinergic system induced by DM232 could make it able to prevent amnesia induced by an antimuscarinic drug as well as by the administration of a nicotinic antagonist. The modulation of the cholinergic system was also postulated as the mechanism of action of the piracetam-like nootropic drugs [Pepeu and Spignoli, 1989]. In particular, it has been reported that piracetam might alter presynaptic cholinergic functions, possibly by enhancing highaffinity neuronal uptake of choline [Pedata et al, 1984], but these data are still a matter of controversy [Franklin et al, 1986].…”

Section: Discussionmentioning

confidence: 99%

The novel nootropic compound DM232 (UNIFIRAM) ameliorates memory impairment in mice and rats

Ghelardini

Galeotti

Gualtieri

et al. 2002

Drug Development Research

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The favorable pharmacological profile exhibited by piracetam stimulated the synthesis of related compounds potentially endowed with a higher nootropic potency. The antiamnesic and procognitive activity of DM232 (unifiram), a new compound structurally related to piracetam, was investigated. Mouse passive avoidance and rat Morris water maze and Social learning tests were employed. DM232 (0.001-1 mg kg À1 i.p. -0.01-0.1 1 mg kg À1 p.o.) prevented amnesia induced by scopolamine (1.5 mg kg À1 i.p.), mecamylamine (20 mg kg À1 i.p.), baclofen (2 mg kg À1 i.p.), and clonidine (0.125 mg kg À1 i.p.). Furthermore, The antiamnesic effect of the investigated compound was comparable to that exerted by well-known nootropic drugs such as piracetam (30-100 mg kg À1 i.p.), aniracetam (100 mg kg À1 p.o.), rolipram (30 mg kg À1 p.o.), and nicotine (5 mg kg À1 i.p). DM232 (0.1 mg kg À1 i.p.) was also able to prevent amnesia induced by scopolamine (0.8 mg kg À1 i.p.) in the rat Morris watermaze test. In the rat social learning test, DM232 (0.1 mg kg À1 i.p.) injected in adults rats reduced the duration of active exploration of the familiar partner in the second session of the test. DM232, similarly to piracetam, reduced the duration of hypnosis induced by pentobarbital. At the highest effective doses, the investigated compound did not impair motor coordination (rota rod test), nor modified spontaneous (Animex). These results indicate DM232 (unifiram) as a novel cognition enhancer, strictly related to piracetam-like compounds, able to ameliorate memory impairment at doses about 1,000 times lower than the most active available nootropic compounds. Drug Dev.

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Nootropic drugs and brain cholinergic mechanisms

Cited by 64 publications

References 50 publications

Effects of Ginsenoside Rbi on Central Cholinergic Metabolism

Effects of Ginsenoside Rbi on Central Cholinergic Metabolism

Ionotropic Glutamate Receptor Modulation of 5-HT6 and 5-HT7 mRNA Expression in Rat Brain

The novel nootropic compound DM232 (UNIFIRAM) ameliorates memory impairment in mice and rats

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