Cognition activators

Moos, Walter H.; Davis, Robert E.; Schwarz, Roy D.; Gamzu, Elkan

doi:10.1002/med.2610080303

Cited by 98 publications

(40 citation statements)

References 405 publications

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“…As depicted in Scheme 1, the key intermediate, 5-(4-chloro- [1,2,5]thiadiazole-3-yl)pyrimidine 4 was prepared as described in our previous paper [12].The starting material, 5-pyrimidinecarboxaldehyde 1 was synthesized from 4,6-dihydroxypyrimidine according to the known procedure [13]. The resultant 4 was treated with KCN/ AcOH to give the cyanohydrin 2 and then subsequent treatment with NH 4 Cl/NH 4 OH in hot acetonitrile yielded the aminonitrile 3.…”

Section: Scheme 1 Synthesismentioning

confidence: 99%

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Synthesis of 5-(4-Alkylsulfanyl-[1, 2, 5]Thiadiazol-3-yl)-3-Methyl-1, 2, 3, 4-Tetrahydropyrimidine Oxalate Salts and their Evaluation as Muscarinic Receptor Agonists

Park

Lee

Kong

et al. 2003

Arch. Pharm. Pharm. Med. Chem.

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The synthesis and biological test of 5-(4-alkylsulfanyl-[1, 2, 5]thiadiazol-3-yl)-3-me-thyl-1, 2, 3, 4-tetrahydropyrimidine oxalate salts 7 as muscarinic receptor agonists are described. The key intermediate 4 was obtained by a modified Strecker reaction and cyclization, and the 3-methyl-1, 2, 3, 4-tetrahydropyrimidines were obtained by subsequent substitution, quarternization, and reduction. The final products 7 were obtained as oxalic acid salts. The prepared compounds were examined in vitro for their binding affinities to the cloned human muscarinic receptor by the [(3)H]-NMS binding assay.

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Section: Scheme 1 Synthesismentioning

confidence: 99%

“…Recent work on Alzheimer's disease (AD) has focused on the development of M 1 -selective agonists [1,2]. M 1 muscarinic receptors play a role in memory function [3,4] and stimulate phosphoinositide (PI) turnover in the mammalian forebrain [5].…”

Section: Introductionmentioning

confidence: 99%

Synthesis of 5-(4-Alkylsulfanyl-[1, 2, 5]Thiadiazol-3-yl)-3-Methyl-1, 2, 3, 4-Tetrahydropyrimidine Oxalate Salts and their Evaluation as Muscarinic Receptor Agonists

Park

Lee

Kong

et al. 2003

Arch. Pharm. Pharm. Med. Chem.

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“…Non-cognitive (BPSD) symptoms are described above, and cognitive symptoms may be defined as those that involve changes in the process of ''knowing'' including both awareness (vigilance) and judgement, or as those involving changes in the analysis and interpretation of events, which would include reasoning and remembering. The dementia that occurs in the elderly and that may be termed ''senile cognitive decline'' involves not only a loss of short-term memory (i.e., anterograde amnesia), which is a cognitive symptom, but also decreases in ''motivation'' which may, at least in some cases, be considered to be a noncognitive (BPSD-type) symptom [see e.g., Moos et al, 1988]. Also, the term ''vigilance'' may be defined as being either non-cognitive or cognitive, depending upon the exact conditions under which it is employed [see e.g., Wilken et al, 2002;Farrin et al, 2002].…”

Section: Effects Of Egb 761 On Behavioral and Psychological Symptoms mentioning

confidence: 99%

“Stress‐alleviating” and “vigilance‐enhancing” actions of Ginkgo biloba extract (EGb 761)

DeFeudis¹,

Drieu

2004

Drug Development Research

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This overview is focused on the stress-alleviating and vigilance-enhancing properties of Ginkgo biloba extract (EGb 761) that have been observed in animal models and in humans and that appear useful in explaining the therapeutic effects of the extract on non-cognitive brain functions that may be reflective of mood changes. With regard to its stress-alleviating activity, in rodents EGb 761 facilitates behavioral adaptation, decreases circulating levels of corticosterone, catecholamines, ACTH, and CRH, suppresses the expression of the mitochondrial peripheral benzodiazepine receptor of the adrenal cortex, increases the anxiolytic activity of diazepam, increases arousal by an action that may involve GABA A receptor antagonism, induces anxiolytic-like activity, prevents stress-induced desensitization of hippocampal 5-HT 1A receptors, suppresses the down-regulation of hippocampal glucocorticoid receptors, and facilitates decision-making. In humans, EGb 761 has vigilance-enhancing effects that support its clinical use in treating disorders involving stress-induced brain dysfunction and those non-cognitive symptoms of dementia currently classified as ''behavioral and psychological symptoms of dementia'' (BPSD). Collectively, these findings indicate that EGb 761 is useful for treating symptoms that are now classified as components of BPSD. As drug combinations consisting of EGb 761 and a non-selective cholinesterase inhibitor, an antidepressant drug, or a neuroleptic could possibly be even more useful in treating BPSD, evaluation of such therapy is recommended. Drug Dev.

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“…Nos últimos anos, tem se usado, com sucesso exíguo e muito variável, uma família de drogas muito atóxicas chamadas nootrópicos (piracetam, vincamina e derivados). Em geral, seu efeito não é melhor que o de um placebo; mas as empresas que as produzem advogam entusiásticamente por seu emprego (MOOS et al, 1988). O futuro da farmacologia da memória, porém, não parece passar por essa família heterogênea de drogas (IZQUIERDO, 1989).…”

Section: Amnésiasunclassified

Memórias

Izquierdo

1989

Estud. av.

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Memórias Ivan IzquierdoO tempo flui, como um rio, aquele ao qual Heráclito disse que não podemos descer duas vezes. Há, basicamente, duas maneiras de conceber o fluxo do tempo: desde o passado em direção ao futuro, ou desde o futuro em direção ao passado (BORGES, 1960). Em qualquer um dos casos, o fluxo nos atravessa num ponto, que denominamos presente. Um ponto não tem superfície nem volume; é intangível e fugaz. É curioso que, em ambas concepções do tempo, o futuro (ou o passado) sejam conseqüências de algo quase imaterial como é o presente; de um simples ponto. Esse ponto evanescente, porém, é nossa única posse real: o futuro não existe ainda (e a palavra ainda é uma petição de princípio) e o passado não mais existe, salvo sob a forma de memórias. Não há tempo sem um conceito de memória; não há presente sem um conceito do tempo; não há realidade sem memória e sem uma noção de presente, passado e futuro.

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Cognition activators

Cited by 98 publications

References 405 publications

Synthesis of 5-(4-Alkylsulfanyl-[1, 2, 5]Thiadiazol-3-yl)-3-Methyl-1, 2, 3, 4-Tetrahydropyrimidine Oxalate Salts and their Evaluation as Muscarinic Receptor Agonists

Synthesis of 5-(4-Alkylsulfanyl-[1, 2, 5]Thiadiazol-3-yl)-3-Methyl-1, 2, 3, 4-Tetrahydropyrimidine Oxalate Salts and their Evaluation as Muscarinic Receptor Agonists

“Stress‐alleviating” and “vigilance‐enhancing” actions of Ginkgo biloba extract (EGb 761)

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