Mutations of the Caenorhabditis elegans dystrophin/utrophin-like dys-1 gene lead to hyperactivity and hypercontraction of the animals. In addition dys-1 mutants are hypersensitive to acetylcholine and acetylcholinesterase inhibitors. We investigated this phenotype further by assaying acetylcholinesterase activity. Total extracts from three different dys-1 alleles showed significantly less acety...

A chemiluminescence method for determining acetylcholinesterase activity is described. It is an adaptation of the chemiluminescence assay of acetylcholine described by Israël & Lesbats [(1981) Neurochem. Int. 3, 81-90; (1981) J. Neurochem. 37, 1475-1483]. The acetylcholinesterase activity is measured by monitoring the increase in light emission produced by the accumulation of choline or by dete...

An electrophoretically mediated microanalysis technique was developed for the rapid screening of acetylcholinesterase inhibitors. Activity of four original compounds, N-benzylpiperidine, carbamoyloxyphenyl derivatives and reference inhibitor--tacrine was determined and compared with the data obtained from Ellman's assay. Percentage of enzyme inhibition detected at inhibitor concentration of 3.3...

The serotonin-sensitive aryl acylamidase was partially purified from monkey brain. The aryl acylamidase activity was inhibited by serotonin (Ki = 0.425 mM) and tryptamine (Ki = 3.6 mM) but not by a number of other amines. It was also inhibited by acetylcholine (Ki = 2 mM) and its analogues and homologues. The relationship of aryl acylamidase to acetylcholinesterase was examined. The ratios of s...

Of the many causes of dementia, Alzheimer disease (AD) is most common. Diagnosis generally followed by treatment. One common treatments AD a type medication called acetylcholinesterase inhibitors (ChEIs). ChEIs work blocking breakdown chemical in brain acetylcholine. In doing so, allows more this to be available brain. This can improve or maintain cognition and memory.

Acetylcholinesterase (AChE), hydrolyzes acetylcholine to choline and acetate, thereby terminating this neurotransmitter effect at cholinergic synapses. Therefore, AChE inhibition is used for counterbalance the deficit in Alzheimer’s disease (AD) patients. In present work, order find new plant acetylcholinesterase inhibitors, hydroalcoholic extracts from seventeen medicinal species were screened...

Three man synthetic routes to analogues of tacrine are described: reaction of anthranilonitriles with cyclohexanone and other ketones, reaction of various anilines with alpha-cyanoketones, and reactions involving anilines and cyclic beta-ketoesters. Although tacrine has a wide range of pharmacological effects, it is best known as an inhibitor of cholinesterase enzymes. Many of the analogues tha...

We previously reported that acetylcholinesterase plays a critical role in apoptosis and its expression is regulated by Ca(2+) mobilization. In the present study, we show that activated calpain, a cytosolic calcium-activated cysteine protease, and calcineurin, a calcium-dependent protein phosphatase, regulate acetylcholinesterase expression during A23187-induced apoptosis. The calpain inhibitor,...

The distribution of acetylcholinesterase in the canine kidney was studied by the histochemical method of Karnovsky and Roots and compared to the distribution of adrenergic fibers studied with the fluorescence histochemical method of Falck and Hillarp. Specific inhibitors of nonspecific cholinesterase and acetylcholinesterase were used to differentiate between the two enzymes. In the hilus, acet...