Dementia is a common symptom of many degenerative brain diseases. The cholinesterase inhibitors are widely recommended for the treatment of Alzheimer’s disease and different kind of dementia to improve memory functions. Tacrine is the first drug from this group. Metrifonate has been used as an antihelminthic in tropical countries for more than 30 years, and even recently has been suggested as a...

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...

AIM To find if tacrine exerts a sensitizing effect on the cholinergic receptors of gastric smooth muscles, and study some of the mechanisms inducing it and measure the relative intensity of tacrine's effects on contractile activity. MATERIAL AND METHODS Isometric recording of the mechanical activity of gastric smooth muscle preparations; determination of acetyl-cholinesterase activity in smoo...

This work presents a novel fluorescent sensor for the determination of tacrine by combining the magnificent fluorescence properties of nitrogen-doped graphene quantum dots (N-GQDs) with the high potential of acetylcholinesterase (AChE) enzyme for screening its inhibitors. Tacrine was the first drug approved for Alzheimer's disease and it is currently being used in several therapeutic treatments...

OBJECTIVE To review systematically the methodology, results and quality of clinical trials of tacrine in the treatment of Alzheimer's disease (AD). METHODS Trials included were those conducted on AD patients, aged 40 years or over, assigned to tacrine- or placebo-based treatment. Studies were identified via the Cochrane Collaboration and MEDLINE databases. Trial-selection and data-extraction ...

A new tacrine based cholinesterase inhibitor, N-(bromobut-3-en-2-yl)-7-methoxy-1,2,3,4-tetrahydroacridin-9-amine (1), was designed and synthesized to interact with specific regions of human acetylcholinesterase and human butyrylcholinesterase. Its inhibitory ability towards cholinesterases was determined and compared to tacrine (THA) and 9-amino-7-methoxy-1,2,3,4-tetrahydroacridine (7-MEOTA). T...

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...

alzheimer's disease (ad) is a progressive neurodegenerative disease characterized by memory and cognitive dysfunction due to neuronal cell loss in higher brain centers. senile plaques containing amyloid β (aβ) are associated with this disease as well as a reduction in cholinergic neuron numbers. tacrine is a reversible cholinesterase inhibitor in clinical use to treat moderate forms of ad. chit...

The use of tacrine-extended suxamethonium in 117 cases is described. The extent of the myoneural block was monitored with the aid of a nerve stimulator. In patients in whom an intubating dose of suxamethonium unaccompanied by tacrine produced a somewhat prolonged apnoea, there was a significant but relatively unimportant prolongation of the action of tacrine-extended suxamethonium. Dual block d...