Nit 153-08 - acetylcholinesterase inhibitors

It is estimated that by 2050, 19 million people in the
more developed countries will be over 65 years old.
At least 50% of them are expected to develop some
form of Alzheimer's disease.

Research into
potential targets
Preclinical research
Clinical research
Semi-synthetic derivatives of plant extracts that act as Inhibit the AChE enzyme to increase the cholinergic activity of acetylcholinesterase (AChE) enzyme inhibitors. They can be the Central Nervous System, controlling the symptoms of used for the treatment of degenerative neuropathies such as Alzheimer's disease in the areas of learning and memory. Alzheimer's and Parkinson's diseases, as well as other Through this mechanism it is also possible to control muscle disorders related to cholinergic transmission, such as paralysis caused by chemical or biological agents, Myasthenia Myasthenia gravis, chemical-related muscle paralysis, gravis and scopolamine poisoning.
scopolamine intoxication, and other pathologies associated The vegetable species in question is endemic to the Atlantic Forest and its extracted compounds may yield 4% in alcohol Alzheimer's disease (AD) is a disorder with a high extract. In in vivo assays, these compounds have been found socioeconomic impact, accounting for 1.70% of deaths in to inhibit the enzyme AChE completely (100%) when developed countries. It is estimated that 24.3 million people compared with the reversible inhibitor galantamine. are affected and that 4.6 million new cases will be reported They are also able to reverse amnesia induced experimental y by scopolamine, unlike tacrine and Alzheimer's is the fifth leading cause of death in developed galantamine. The compounds do not present the toxic effects countries, taking the lives of 168 thousand people per year reported for the two commercial drugs used in preclinical In the U.S., 10.9 million people are unpaid caregivers. Most of these caregivers are close relatives of the patient, which causes a heavy emotional and financial burden on families as the disease progresses, ending in death. From the early symptoms to death, the progression of the disease is 8.5 to 11 years, with an average life expectancy of 4 to 6 years In 2009, two of the main drugs for the treatment of Alzheimer's (Alzheimer's Assoc., 2010). The estimated global cost of disease, rivastigmine and donepezil, both AChE inhibitors, treating Alzheimer's is approximately US$ 315 billion (Pfizer , reached sales of US$ 954 million and US$ 432 million, respectively. There is a high demand for new drugs, as indicated by the R&D lines on Alzheimer's of the major players in the pharmaceutical industry. In Brazil, the federal Exceptional Medicines Program and that of several state governments covers the costs of medications for pathologies such as Alzheimer's. The budget increase from 2004 to 2008 was 345%, corresponding to R$ 2.3 billion last year.
UNESP Technology Transfer Office - AUIN
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NJSIAA Banned-Drug Classes 2012 - 2013 The term “related compounds” comprises substances that are included in the class by their pharmacological action and/or chemical structure. No substance belonging to the prohibited class may be used, regardless of whether it is specifically listed as an example. Many nutritional/dietary supplements contain NJSIAA banned substances. In additi

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