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

Amenta, Francesco; Tayebati, Seyed Khosrow; Vitali, Daniela G.; Tullio, Maria Antonietta Di

doi:10.1016/j.mad.2005.09.017

Cited by 43 publications

(39 citation statements)

References 28 publications

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“…A choline-containing phospholipid recently revisited both in preclinical and clinical investigations is GPC. Treatment with GPC alone or in association with the cholinesterase inhibitor rivastigmine significantly increased ACh concentrations in different rat cerebral areas (cerebral cortex, hippocampus, and striatum) [ 66 ]. The results regarding cerebral cortex can be observed in Figure 4 .…”

Section: Treatment With Cdp-choline and Gpc: Pre-clinical And Clinicamentioning

confidence: 80%

Choline-containing phospholipids: relevance to brain functional pathways

Tayebati

Amenta

2013

Clinical Chemistry and Laboratory Medicine

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Choline participates in several relevant neurochemical processes. It is the precursor and metabolite of acetylcholine (ACh), plays a role in single-carbon metabolism and is an essential component of different membrane phospholipids (PLs). PLs are structural components of cell membranes involved in intraneuronal signal transduction. This paper reviews the roles of choline and of choline-containing phospholipids (CCPLs) on brain metabolism in health and disease followed by an analysis of the effects of exogenously administered CCPLs on the brain, a topic extensively investigated by literature. Based on the observation of decreased cholinergic neurotransmission in brain disorders characterized by cognitive impairment, cholinergic precursor loading therapy with CCPLs was the first approach used to attempt for relieving the cognitive symptoms of Alzheimer ' s disease. This therapeutic strategy was discontinued due to the negative clinical results obtained with choline or lecithin. Negative results obtained with some compounds cannot be generalized for all CCPLs, as CDP-choline (citicoline) and to a greater extent choline alphoscerate (GPC) displayed interesting effects documented in preclinical studies and limited clinical trials. We provide evidence in favor of CDP-choline and GPC activity in cerebrovascular or neurodegenerative disorders characterized by cholinergic neurotransmission impairment. Based on the results of the controlled clinical trials available, we suggest that due to the lack of novel therapeutic strategies, safe compounds developed a long time ago such as effective CCPLs could have still a place in pharmacotherapy. Therefore selected compounds of this class should be further investigated by new appropriate clinical studies.

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Section: Treatment With Cdp-choline and Gpc: Pre-clinical And Clinicamentioning

confidence: 80%

Choline-containing phospholipids: relevance to brain functional pathways

Tayebati

Amenta

2013

Clinical Chemistry and Laboratory Medicine

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“…Choline alphoscerate (L-alpha-glyceryl-phosphoryl-choline, is a cholinergic precursor studied both in preclinical paradigms and in clinical trials [14][15][16]. This compound increases acetylcholine release in rat hippocampus and improves memory and attention, as well as affective and somatic symptoms (fatigue, vertigo) in VaD patients [17].…”

Section: Introductionmentioning

confidence: 99%

“…Studies of our group have reported that combination choline alphoscerate with the AChE/ChE inhibitor rivastigmine may represent an association enhancing cholinergic neurotransmission more effectively than single compounds [16]. This association was proposed as a possible strategy for replacement therapy in pathologies characterized by altered cholinergic neurotransmission [16].…”

Section: Introductionmentioning

confidence: 99%

Neuroprotective effect of treatment with galantamine and choline alphoscerate on brain microanatomy in spontaneously hypertensive rats

Tayebati

Tullio

Tomassoni

et al. 2009

Journal of the Neurological Sciences

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“…Оригинальный препарат этой группы (Глиатилин) длительно изучался в международных ран-домизированных плацебо-контролируемых исследова-ниях и обладает достаточной доказательной базой, позволяющей свидетельствовать о доказанной эффек-тивности его использования в комбинированной тера-пии БА [2][3][4][5][6].…”

Section: для дополнительного усиления действия ингибиторов ацетилхолиunclassified

“…Полученный холин проникает через гематоэнцефалический барьер и попа-дает в головной мозг, где служит основой для образова-ния ацетилхолина. Глицерофосфат, являясь предшествен-ником фосфолипидов мембраны нейронов, стимулирует образование фосфатидилхолина, который восстанавли-вает фосфолипидный состав мембран нейронов и улуч-шает их пластичность [4][5][6].…”

Section: для дополнительного усиления действия ингибиторов ацетилхолиunclassified

Modern Approaches to Diagnostics and Therapy of Alzheimer Disease

Преображенская¹

2017

Med. sov.

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В статье приведены современные данные о причинах развития, методах диагностики и подходах к лечению болезни Альцгеймера. Особое внимание уделено патогенетической и симптоматической терапии этого заболевания, а также неле-карственным методам лечения. I.S. PREOBRAZHENSKAYA, MD, Prof., Sechenov First Moscow State University of the Ministry of Health of Russia MODERN APPROACHES TO DIAGNOSTICS AND THERAPY OF ALZHEIMER DISEASEThe article presents modern data on the causes of development, diagnostic methods and treatment approaches of Alzheimer's disease. Special attention is given to pathogenetic and symptomatic therapy of this disease, as well as non-drug treatments.

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

Cited by 43 publications

References 28 publications

Choline-containing phospholipids: relevance to brain functional pathways

Choline-containing phospholipids: relevance to brain functional pathways

Neuroprotective effect of treatment with galantamine and choline alphoscerate on brain microanatomy in spontaneously hypertensive rats

Modern Approaches to Diagnostics and Therapy of Alzheimer Disease

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