Association with the cholinergic precursor choline alphoscerate and the cholinesterase inhibitor rivastigmine: an approach for enhancing cholinergic neurotransmission.

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Amenta F, Tayebati SK, Vitali D, Di Tullio MA

Association with the cholinergic precursor choline alphoscerate and the cholinesterase inhibitor rivastigmine: an approach for enhancing cholinergic neurotransmission.

Mech Ageing Dev. 2006 Feb;127(2):173-9. Epub 2005 Nov 16.

PubMed ID
16297435 [ View in PubMed
]
Abstract

The effects of association of cholinergic precursors choline or choline alphoscerate with the cholinesterase inhibitor rivastigmine on acetylcholine levels and [(3)H]hemicholinium-3 binding were assessed in rat frontal cortex, hippocampus and striatum. Acetylcholine immunoreactivity was also evaluated in cerebrocortical cholinergic fibers by immunohistochemistry. Choline alphoscerate or rivastigmine, but not choline increased acetylcholine levels as well as [(3)H]hemicholinium-3 binding used as a marker of high affinity cholinergic transporter. The association of choline alphoscerate with rivastigmine dose-dependently increased both acetylcholine levels and [(3)H]hemicholinium-3 binding. Rivastigmine alone or in association with either choline or choline alphoscerate decreased acetylcholinesterase (AChE), whereas choline or choline alphoscerate alone did not affect AChE activity. Choline alphoscerate or rivastigmine alone or in association, but not choline increased acetylcholine immunoreactivity in nerve fibers supplying cerebral cortex. These data suggest that combination of a suitable precursor of brain acetylcholine such as choline alphoscerate and of a cholinesterase inhibitor may represent an association worthwhile of being further investigated as a cholinergic replacement therapy in pathologies characterized by altered cholinergic neurotransmission.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
CholineAcetylcholinesteraseProteinHumans
Unknown
Product of
Details
CholineCholinesteraseProteinHumans
Unknown
Product of
Details
Choline salicylateAcetylcholinesteraseProteinHumans
Unknown
Product of
Details
Choline salicylateCholinesteraseProteinHumans
Unknown
Product of
Details