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3.
J Pharm Pharmacol ; 70(8): 985-993, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29663387

RESUMO

OBJECTIVES: Alzheimer's disease (AD) has become the primary cause of dementia. It shows a progressive cognitive dysfunction with degenerating neurons. Acetylcholine receptors (AChRs) propagate the cognitive ability and it consists of two primary members namely muscarinic (mAChRs) and nicotinic receptors (nAChRs). Where mAChRs is G-protein coupled receptor, (nAChRs) are ligand-gated ion channels. The conventional therapeutic regimen for AD consists of three acetylcholinestearse inhibitors while a single NMDA receptor antagonist. Researchers around the globe are developing new and modifying the existing AChRs agonists to develop lead candidates with lower risk to benefit ratio where benefits clearly outweigh the adverse events. KEY FINDINGS: We have searched PubMed, MEDLINE, Google scholar, Science Direct and, Web of Science with keywords "Muscarinic/Nicotinic acetylcholine receptor, agonists and, AD". The literature search included articles written in English. Scientific relevance for clinical studies, basic science studies is eligibility criteria for articles referred in this paper. M1 is the primary muscarinic subtype while α7 is the primary nAChR subtype that is responsible for cognition and memory and these two have been the major recent experimental targets for mAChR agonist strategy. SUMMARY: The last cholinergic receptor agonist to enter phase 3 trial was EVP-6124 (Enceniclin) but was withdrawn due to severe gastrointestinal adverse effects. We aim to present an overview of the efforts and achievements in targeting Muscarinic and Nicotinic acetylcholine receptor in the current review for development of better AD therapeutics.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Agonistas Muscarínicos/uso terapêutico , Agonistas Nicotínicos/uso terapêutico , Receptores Muscarínicos/metabolismo , Receptores Nicotínicos/metabolismo , Regulação Alostérica/efeitos dos fármacos , Doença de Alzheimer/metabolismo , Animais , Ensaios Clínicos como Assunto , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos , Humanos , Ligação Proteica
4.
Electrophoresis ; 38(6): 820-832, 2017 03.
Artigo em Inglês | MEDLINE | ID: mdl-27921314

RESUMO

Flavonoids represent an important bioactive component in plants. Accumulation of flavonoids often occurs in plants subjected to abiotic stresses, including the adaptation of plants to the environment and in overcoming their stress conditions. This fact makes their analysis and determination an attractive field in food science since they can give interesting information on the quality and safety of foods. In this study, we discuss reports on plants flavonoids biosynthesis against abiotic stresses and advances in analytical capillary electrophoresis used for their identification and quantification in plants.


Assuntos
Eletroforese Capilar/métodos , Flavonoides/análise , Flavonoides/biossíntese , Plantas/química , Qualidade dos Alimentos , Inocuidade dos Alimentos , Humanos , Extratos Vegetais/química , Folhas de Planta/química
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