The long-term studies of the cholinesterase inhibitors, Aricept (donepezil), Razadyne (galantamine) and Exelon (rivastigmine), support their ability to delay Alzheimer’s disease (AD) progression during the dementia stage by 1, 1.5, and 2.5 years respectively, which underscores the importance of early detection to optimize quality of life. Cholinesterase inhibitors reduce caregiving burden by de...

Human cholinesterase exists in two forms--acetylcholinesterase located in tissue microsomes and red blood cells and serum cholinesterase found in serum or plasma. The two enzymes display marked differences in structure, substrate specificity, biological function, and origin. Contemporary methods employ acylthiocholine as substrate for serum cholinesterase and a second coupled reaction of thioch...

The activity and properties of cholinesterase of the motor end plate in human intercostal muscle were studied in the isolated muscle membrane. This preparation was used because cholinesterase activity of the membrane preparation was localized in the motor end plate without contamination of cholinesterase of other muscle components. Under the experimental conditions, cholinesterase in a human en...

The impact of behavioral symptoms associated with Alzheimer's disease is substantial. These symptoms contribute to diminished quality of life for patients and caregivers and increase the cost of care in nursing homes. Early recognition of behavioral symptoms and appropriate treatment are important for successful management. Nonpharmacologic strategies remain the cornerstone of the management of...

Previous investigators (Frawley, Hagan & Fitzhugh, 1952; Davison, 1955; Kewitz & Nachmansohn, 1957) have observed that the rate of recovery in vivo of inhibited brain true cholinesterase depended on which inhibitor was used. With diiwopropyl phosphorofluoridate (Frawley et al. 1952; Davison, 1955; Kewitz & Nachmansobn, 1957) recovery was slow, whereas with tetraethyl pyrophosphate (Davison, 195...

Rutaecarpine is a pentacyclic indolopyridoquinazolinone alkaloid found in Evodia rutaecarpa and other related herbs. It has a variety of intriguing biological properties, which continue to attract the academic and industrial interest. Studies on rutaecarpine have included isolation from new natural sources, development of new synthetic methods for its total synthesis, the discovery of new biolo...

Cholinomimetic drugs can elicit some or all of the effects that acetylcholine (ACh) produces. This class of drugs includes agents that act directly as agonists at cholinoreceptors and agents that act indirectly by inhibiting the enzymatic destruction of endogenous ACh (i.e., cholinesterase inhibitors).The directly acting cholinomimetics can be subdivided into agents that exert their effects pri...