31 results about "Acetyl cholinesterase" patented technology

A method for treating the adverse effects of acetyl-cholinesterase inhibitors used in the treatment of cognitive disorders such as acute delirium and cognitive impairment in elderly human patients. The administration of a clinically effective amount of a quaternary ammonium anti-cholinergic muscarinic receptor antagonist having very low lipid solubility substantially eliminates the adverse effects of urinary and / or fecal incontinence, nausea, bradycardia, bronchorrhea or brochospasm caused by the acetyl-cholinesterase inhibitors, without affecting the beneficial activity of the acetyl-cholinesterase inhibitors. This permits the administration of the optimum effective dosing of acetyl-cholinesterase inhibitors to provide maximum benefit to the patient with the added benefit of reducing or eliminating the unwanted side effects of fecal and urinary incontinence. Further, the combination of rivastigmine and glycopyrrolate has been effective in significantly improving cognitive function in patients suffering from acute dementia or cognitive impairment.

A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.

A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.

There is disclosed a method of treating various diseases caused by micro-vasculature circulation problems, including, but not limited to, vascular insufficiency, phantom pain, diabetic neuropathy, neuropathic pain, autoimmune / inflammatory diseases (e.g., multiple sclerosis, Parkinson's disease, Crohn's Disease, lupus, rheumatoid arthritis, polymyalgia rheumatica, polymyositis, dermatomyositis, sarcoidosis), urinary retention, lymphoedema, and chronic renal insufficiency. Specifically, there is disclosed a treatment providing an effective amount of an acetyl cholinesterase inhibitor compound (or combination of compounds) to treat one or a plurality of microvasculature diseases.

The invention belongs to the medicine field, and relates to tacrine-pyridinothiophene compounds and applications thereof. The saccharides of tacrine-pyridinothiophene compounds have activity on inhibiting kinase-3beta acetyl cholinesterase dual targets. The compounds can be used as a precursor for preventing Alzheimer's disease by inhibiting the activity of cholinesterase.

The invention discloses a Chinese medicinal formulation for preventing and treating senile dementia and a production method thereof. The invention is characterized in that the Chinese medicinal formulation is made from the following Chinese medicinal raw materials in parts by weight: 3-15 of Arillus longan pulp, 3-15 of Polygonum multiflorum and 3-15 of mulberry. The Chinese medicinal formulation has the effects of tonifying the kidney-essence, promoting blood circulation, removing blood stasis, nourishing the heart, soothing the mind and regulating the activity of acetylcholinesterase in the brain cholinergic nerve system; and can be used for prevention and treatment of senile dementia, manifested by symptoms of amnesia, insomnia, hypomnesia and change of activity of brain acetylcholinesterase (AchE) with good efficacy.

The invention relates to the field of quick detection of food safety, in particular to a pesticide residue detection method and a detection kit. The method comprises the following steps: S1, embedding: embedding silk fibroin and acetylcholin esterase into a multi-hole substrate to repaper an enzyme substrate; S2, sample preparation: uniformly mixing a sample to be detected with a buffer solution to obtain a sample solution; S3, detection: adding the sample solution to the enzyme substrate for incubation, then adding an acetyl cholinesterase substrate for incubation for a period of time, and detecting the mixture to obtain a pesticide residue result in the sample to be detected by adopting a pH method, a potentiometric titration method, a manometric method or a colorimetric method. The kit comprises the multi-hole substrate embedded with the silk fibroin and the acetylcholin esterase, the buffer solution and an acetyl cholinesterase substrate solution. The pesticide residue detection method and the detection kit are used for detecting organophosphorus and carbamate insecticides, and are low in detection cost, high in stability and high in sensitivity.

A group of indolealkylamino-withasteroid conjugates, isolated and purified from Withania somnifera, are described. A synthetic method of making an indolealkylamino-withasteroid compound is provided. In vitro acetyl cholinesterase inhibitory activity and methods for treatment of dementia and dementia-related disorders, such as Alzheimer's disease, and anxiety and depressive disorders in mammals are demonstrated with these novel compositions.

A method for treating the adverse effects of acetyl-cholinesterase inhibitors used in the treatment of cognitive disorders such as acute delirium and cognitive impairment in elderly human patients. The administration of a clinically effective amount of a quaternary ammonium anti-cholinergic muscarinic receptor antagonist having very low lipid solubility substantially eliminates the adverse effects of urinary and / or fecal incontinence, nausea, bradycardia, bronchorrhea or brochospasm caused by the acetyl-cholinesterase inhibitors, without affecting the beneficial activity of the acetyl-cholinesterase inhibitors. This permits the administration of the optimum effective dosing of acetyl-cholinesterase inhibitors to provide maximum benefit to the patient with the added benefit of reducing or eliminating the unwanted side effects of fecal and urinary incontinence. Further, the combination of rivastigmine and glycopyrrolate has been effective in significantly improving cognitive function in patients suffering from acute dementia or cognitive impairment.

The invention discloses a piperazine compound and application of the piperazine compound served as a calcium channel blocker or / and an acetyl cholinesterase inhibitor.

The invention discloses 7H-benzo-isoxazole-[7,6-e][1,3]oxazine derivatives as shown in the formula I or pharmaceutically acceptable hydrates / salts thereof, and further discloses stereoisomers or tautomers of the 7H-benzo-isoxazole-[7,6-e][1,3]oxazine derivatives. According to the formula I, R1 represents a hydrogen group, a methyl group, an ethyl group, a halogen group, a methoxyl group, an ethoxy group, a nitro group or an alkoxyl group. The 7H-benzo-isoxazole-[7,6-e][1,3]oxazine derivatives have an obvious effect in inhibiting acetyl cholinesterase, and can be used for enhancing the memory of patients suffering from dementia and the Alzheimer's disease. The invention further relates to preparation methods of the derivatives and application of the derivatives to preparation of medicine used for treating the Alzheimer's disease.

The invention adopts a virtual medicine screening technology and a high-throughput screening technology, assesses the AChE inhibitory activity of more than ten thousand samples in a compound sample library and finds a batch of compounds with higher inhibitory activity by establishing a virtual acetylcholinesterase inhibitor screening method and an AChE activity detection method. Then according tothe pathological features of senile dementia, the compounds with higher AChE inhibitory activity are subject to butyryl choline esterase inhibitory activity detection. Research results show that bimolecular 3-piperidyl-ethyl phenyl ketone not only has comparatively high AChE inhibitory activity, but also has very strong BuChE inhibitory activity; the results of animal experiments prove that the bimolecular 3-piperidyl-ethyl phenyl ketone can remarkably improve aphronesia caused by scopolamine and sodium nitrite and can enhance the ability of learning and memory.

The invention discloses a class of carbamate-chalcone cholinesterase inhibitors and a preparation method and application thereof, belonging to the field of medicinal chemistry. The general chemical structure formula of the cholinesterase inhibitor of the present invention is shown in formula (I), wherein A, B, V, X, Y, and Z are as defined in the present invention. The carbamate-chalcone cholinesterase inhibitor of the present invention has stronger acetylcholinesterase inhibitor activity, butyrylcholinesterase inhibitory activity and selective inhibition of butyrylcholinesterase activity, It has lower neurotoxicity and can be applied to the preparation of medicines for treating and preventing diseases caused by cholinesterase.

The invention discloses a piperazine compound and application of the piperazine compound served as a calcium channel blocker or / and an acetyl cholinesterase inhibitor.

The invention relates to the technical field of electrochemical analysis, in particular to an AchE / GQDs / N-F-TiO2Ns photoelectrochemical biosensor preparation method and application thereof. The AchE / GQDs / N-F-TiO2Ns photoelectrochemical biosensor comprises GQDs / N-F-TiO2Ns and AchE, wherein the GQDs / N-F-TiO2Ns comprises a nitrogen and fluorine-doped titanium dioxide nanotube array (N-F-TiO2Ns) and graphene quantum dots (GQDs) modified on the titanium dioxide nanotube array; cross-linking modification of acetyl cholinesterase (AchE) on the GQDs / N-F-TiO2Ns is carried out; the wavelength at the highest photocurrent response of the photoelectrochemical biosensor is 365 nm; and cross-linking modification of the AchE on the GQDs / N-F-TiO2Ns is carried out through chitosan. The modification of the graphene quantum dots improves the photocurrent intensity. Due to the good biocompatibility, the immobilization of the enzyme on an electrode is improved, and the affinity of the enzyme to a substrateis improved at the same time. the method can also be used in detection study related to acetylcholine and acetyl cholinesterase.

The invention relates to the field of biochemical detection, in particular to an organophosphorus detection method based on LSPR (localized surface plasma resonance). According to the method, an organophosphorus sample is sufficiently contacted with an acetyl-cholinesterase immobilized sensing chip, and an organophosphorus inhibiting enzyme film is formed on the surface of the sensing chip; the sensing chip containing the organophosphorus inhibiting enzyme film is immersed into a mixed solution of acetylthiocholine and chloroauric acid for a sufficient reaction, and gold nanoparticles are formed on the surface of the sensing chip; the sensing chip containing the gold nanoparticles is irradiated by visible light or infrared light, and an extinction spectrum of transmission light is measured, and an LSPR spectrum is acquired; the LSPR spectrum is compared with a standard LSPR spectrum, whether the organophosphorus sample contains organophosphorus is determined according to deviation of absorption peak; the concentration of the organophosphorus is determined according to displacement of the absorption peak. Metal nanoparticles are not required to be prepared before the acetyl-cholinesterase film is immobilized, the detection process is simplified, and low cost is realized.

A simple, industrial process for the preparation of the intermediates of acetyl cholinesterase inhibitors is provided. Thus, for example, 5,6-dimethoxy-2-(4-pyridyl)methyl-1-indanone is hydrogenated using platinum oxide catalyst in the presence of hydrochloric acid under a pressure of 2 bars to give 4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, which is then converted to donepezil hydrochloride, an acetyl cholinesterase inhibitor.

Sheet-like pharmaceutical preparations based on hydrophilic polymers, which rapidly disintegrate upon contact with moisture and which are used to treat dementia-related illnesses The dosage form contains an active agent combination of at least two active agents which are suitable for the treatment of dementia (antidementia agents). The antidementia agents should be chosen from the group comprising acetyl cholinesterase inhibitors (AChE inhibitors) and NMDA antagonists (n-methyl-D-asparaginic acid antagonists). The use of such an active agent combination for producing an orally administrable pharmaceutical product for the treatment of dementia-related illnesses such as Alzheimer's disease, as well as a procedure for the symptomatic treatment of Alzheimer's disease by the oral administration of one of the above pharmaceutical products is also provided.

A simple, industrial process for the preparation of the intermediates of acetyl cholinesterase inhibitors is provided. Thus, for example, 5,6-dimethoxy-2-(4-pyridyl)methyl-1-indanone is hydrogenated using platinum oxide catalyst in the presence of hydrochloric acid under a pressure of 2 bars to give 4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrochloride, which is then converted to donepezil hydrochloride, an acetyl cholinesterase inhibitor.

The invention relates to a heterocyclic compound for treating Alzheimer disease and a preparation method thereof. The heterocyclic compound has a good effect of inhibiting the activity of acetyl cholinesterase; as proved by a behavioral experiment research of a senescence-accelerated mouse (SAM-P / 8), the heterocyclic compound can effectively improve the memory function of the SAM-P / 8 mouse, so that the heterocyclic compound can be used for treating cognitive dysfunction and / or neural degeneration dementia with abnormal protein aggregation, particularly the Alzheimer disease.

The present invention provides a kit and a method of testing for carbamates in amine cured epoxies. The method and kit are based on the use of an enzyme that is inhibited by carbamates. A specific embodiment of the kit includes acetylthiocholine (ATC), dithio-bis (2-nitrobenzoic acid) (DTNB), and acetyl-cholinesterase (ACh-E). In the corresponding method embodiment, the method comprises the steps of collecting carbamates from the epoxy, adding the collected carbamates to a solution, adding acetyl-cholinesterase (ACh-E) to the solution, adding acetylthiocholine (ATC) to the solution, adding dithio-bis (2-nitrobenzoic acid) (DTNB) to the solution, and ultimately measuring the intensity of the yellow color of the solution.

Pharmaceutical compositions and combinations containing a muscarinic receptor antagonist, such as oxybutynin in a transdermal therapeutic system, and a muscarinic receptor agonist, optionally with an acetyl cholinesterase inhibitor, and methods of using the same for treatment of hypocholinergic disorders of the central nervous system such as Alzheimer type dementia. The respective pharmaceutical compositions and combinations of the present invention allow for safe administration of high doses of muscarinic receptor agonist, and improved efficacy of the muscarinic receptor agonist for treatment of hypocholinergic disorders of the central nervous system. The pharmaceutical compositions and combinations also allow for a maximum supply of acetylcholine to the central nervous system, when an acetyl cholinesterase inhibitor is used in combination with a muscarinic receptor antagonist and a muscarinic receptor agonist.

The invention discloses a traditional Chinese medicine for preventing and treating senile dementia and a production method, and belongs to the field of traditional Chinese medicines. The traditional Chinese medicine is prepared from radix salviae miltiorrhizae, arillus longan, radix polygoni multiflori (processed) and fructus mori according to the scientific configuration of the combination of thetheory of traditional Chinese medicine, the theory of modern medicine and experiments. The production method comprises the following steps: extracting the above medicines with water, carrying out alcohol precipitation and concentration, preparing powder and preparing oral liquid, granules, capsules and tablets by using modern pharmaceutical production processes. The traditional Chinese medicine has the pharmacological effects of tonifying the kidney and replenishing essence, invigorating blood circulation and removing blood stasis, tranquilizing mind by nourishing the heart, adjusting the activity of acetylcholinesterase and choline acetyl transferase in the cholinergic nervous system of the brain, eliminating oxygen free radicals, discharging aluminum and the like. The traditional Chinese medicine is used for preventing and treating amnesia, insomnia, hypomnesis, activity change of acetylcholinesterase (AchE) and choline acetyl transferase (chAT) of the brain, elimination of oxygen free radicals, discharging aluminum and the like caused by senile dementia.

The invention relates to a heterocyclic compound for treating Alzheimer disease and a preparation method thereof. The heterocyclic compound has a good effect of inhibiting the activity of acetyl cholinesterase; as proved by a behavioral experiment research of a senescence-accelerated mouse (SAM-P / 8), the heterocyclic compound can effectively improve the memory function of the SAM-P / 8 mouse, so that the heterocyclic compound can be used for treating cognitive dysfunction and / or neural degeneration dementia with abnormal protein aggregation, particularly the Alzheimer disease.

A combination of a non-selective, peripheral anticholinergic agent, and a muscarinic receptor agonist, optionally with an acetyl cholinesterase inhibitor, and method of using the same for the treatment of hypocholinergic disorders of the central nervous system. The combination of the present invention allows for safe administration of high doses of muscarinic receptor agonist, and improved efficacy of the muscarinic receptor agonist for treatment of hypocholinergic disorders of the central nervous system. The combination also allows for a maximum supply of acetylcholine to the central nervous system, when an acetyl cholinesterase inhibitor is used in combination with a non-selective, peripheral anticholinergic agent and a muscarinic receptor agonist.

The invention relates to the technical field of traditional Chinese medicine, in particular to a traditional Chinese medicine composition for treating Alzheimer's disease, a preparation method and application thereof. The traditional Chinese medicine composition is prepared from Rehmannia glutinosa, Chinese yam, Poria cocos, Cornus officinalis, Alisma, Cortex Moutan, cinnamon, epimedium, calamus calamus and fennel. The composition provided by the invention, through reasonable compatibility, makes each component produce a synergistic effect, and has remarkable curative effect on Alzheimer's disease. Experimental results show that the traditional Chinese medicine composition provided by the present invention can reduce SH-SY5Y cell damage caused by low sugar and hypoxia, improve the spatial learning ability and spatial exploration ability of Alzheimer's disease rats, and reduce the content of acetylcholinesterase AchE in brain tissue , inhibit the apoptosis of nerve cells in the CAI area, and have a significant therapeutic effect on Alzheimer's disease.

A method administers quaternary ammonium anti-cholinergic muscarinic receptor antagonists in combination with acetyl-cholinesterase inhibitors to treat either cognitive impairment or acute delirium. This therapy results in a modification of a cognitive disorder or disease, namely a slow down in the disease progression. In one preferred embodiment, the disease is dementia with Lewy Bodies. New formulations for quaternary ammonium anti-cholinergic muscarinic receptor antagonists are also disclosed.

Pharmaceutical compositions and combinations containing a muscarinic receptor antagonist, such as oxybutynin in a transdermal therapeutic system, and a muscarinic receptor agonist, optionally with an acetyl cholinesterase inhibitor, and methods of using the same for treatment of hypocholinergic disorders of the central nervous system such as Alzheimer type dementia. The respective pharmaceutical compositions and combinations of the present invention allow for safe administration of high doses of muscarinic receptor agonist, and improved efficacy of the muscarinic receptor agonist for treatment of hypocholinergic disorders of the central nervous system. The pharmaceutical compositions and combinations also allow for a maximum supply of acetylcholine to the central nervous system, when an acetyl cholinesterase inhibitor is used in combination with a muscarinic receptor antagonist and a muscarinic receptor agonist.

A group of indolealkylamino-withasteroid conjugates, isolated and purified from Withania somnifera, are described. A synthetic method of making an indolealkylamino-withasteroid compound is provided. In vitro acetyl cholinesterase inhibitory activity and methods for treatment of dementia and dementia-related disorders, such as Alzheimer's disease, and anxiety and depressive disorders in mammals are demonstrated with these novel compositions.