Monoamines and their Derivatives on GPCRs: Potential Therapy for Alzheimer's Disease
| Autor: | Rodolfo Pinto-Almazán, Martha Cecilia Rosales-Hernández, Marvin A. Soriano-Ursúa, Ricardo Márquez-Gómez, Eunice D. Farfán-García, Teresa Pérez-Capistran, Mónica Barrón-González |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
Amyloid beta Tau protein Neuropathology Receptors G-Protein-Coupled 03 medical and health sciences 0302 clinical medicine Alzheimer Disease medicine Animals Humans Neurochemistry Biogenic Monoamines Amyloid beta-Peptides biology 030104 developmental biology Monoamine neurotransmitter Neurology Mechanism of action Drug Design biology.protein Cholinergic Neurology (clinical) Serotonin medicine.symptom Neuroscience 030217 neurology & neurosurgery |
| Zdroj: | Current Alzheimer research. 16(10) |
| ISSN: | 1875-5828 |
| Popis: | Albeit cholinergic depletion remains the key event in Alzheimer’s Disease (AD), recent information describes stronger links between monoamines (trace amines, catecholamines, histamine, serotonin, and melatonin) and AD than those known in the past century. Therefore, new drug design strategies focus efforts to translate the scope on these topics and to offer new drugs which can be applied as therapeutic tools in AD. In the present work, we reviewed the state-of-art regarding genetic, neuropathology and neurochemistry of AD involving monoamine systems. Then, we compiled the effects of monoamines found in the brain of mammals as well as the reported effects of their derivatives and some structure-activity relationships. Recent derivatives have triggered exciting effects and pharmacokinetic properties in both murine models and humans. In some cases, the mechanism of action is clear, essentially through the interaction on G-protein-coupled receptors as revised in this manuscript. Additional mechanisms are inhibition of enzymes for their biotransformation, regulation of free-radicals in the central nervous system and others for the effects on Tau phosphorylation or amyloid-beta accumulation. All these data make the monoamines and their derivatives attractive potential elements for AD therapy. |
| Databáze: | OpenAIRE |
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