84 results about "Acetyl choline" patented technology

The invention discloses a microelectrode array chip for multi-parameter detection of nerve cells and a preparation method thereof, relating to a sensor technology. The chip consists of seven parts including an insulating base, a microelectrode array, counter electrodes, reference electrodes, electrode leads, contacts, a superficial insulating layer and a modification material, wherein the electrodes are prepared by using a micro-electro-mechanical system (MEMS) process, and a specific nano-composite material and enzymes are modified at fixed points on the surfaces of the electrodes. The nerve cells are cultivated on the surfaces of modified working electrodes, and by combining the counter electrodes and the reference electrodes, the microelectrode array chip can be used for detecting electrophysiological signals of the nerve cells and electrochemical signals of neurotransmitters such as dopamine, acetyl choline and the like in real time at the same time, and has a function of applying electrical stimulation to the nerve cells. The microelectrode array chip integrates functions, modifies a material at fixed points, is convenient to use, and is suitable for culturing the nerve cells and making related research on multi-parameter detection of the nerve cells in laboratories.

The invention discloses a 4'-carbamate derivative of scutellarin shown in formula (I), a preparation method of the compound and application of the compound in preparing medicines for preventing and / or treating various symptoms and diseases caused by acetyl cholinesterase and / or mediated by free radicals, such as vascular dementia and Alzheimer's disease. In the formula, each of R1, R2 and R3 independently represents H, C1-C12 alkyl or R6CO, wherein R6 represents C1-C12 alkyl, but R1, R2 and R3 are not H at the same time; each of R4 and R5 independently represents H, C1-C12 alkyl, C1-C6 fatty alcohol, or an ester formed by the C1-C6 fatty alcohol and C1-C6 carboxylic acid, the C1-C6 carboxylic acid, or an ester formed by the C1-C6 carboxylic acid and the C1-C6 fatty alcohol; or R4NR5 represents a morpholine ring, a piperidine ring, a 4-benzyl piperidine ring, a piperazine ring, the piperazine ring with the 4-position substituted by C1-C12 alkyl, or a tetrahydropyrrole ring.

There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.

PCT No. PCT / SE96 / 01677 Sec. 371 Date Sep. 21, 1998 Sec. 102(e) Date Sep. 21, 1998 PCT Filed Dec. 17, 1996 PCT Pub. No. WO97 / 22339 PCT Pub. Date Jun. 26, 1997This invention relates to a method for treating snoring, sleep apnea and other form of sleep-disordered breathing, which comprises administration of a therapeutically effective dose of an acetyl choline esterase inhibitor (CEI) such as pyridostigmine or a pharmaceutically acceptable salt thereof.

The invention belongs to the field of medicines and chemical industries, and discloses a method for preparing a series of tacrine heterocomplexes and use in medicines for curing neurodegenerative diseases. The invention further relates to use of the tacrine heterocomplex for preparing medicines for curing the neurodegenerative diseases independently or with other medicines. The structural formula of the tacrine heterocomplex is as follows: FORMULA, wherein when X is O or CH2 and Y is N, R1, R2 and R3 are H; n is 2, 3, 4, 5, 6, 8, 9, 10, 11 or 12; when X is O or CH2 and Y is C, R1 is H, OH or OCH3; R2 is H, OH or OCH3; R3 is H, OH or OCH3; R4 is H, OH or OCH3; and n is2, 3, 4, 5, 6, 8, 9, 10, 11 or 12. The tacrine heterocomplex disclosed by the invention has strong inhibitory activity to acetylcholinesterase (AChE) and butyrylcholine esterase (BuChE), which are effectively used for curing the neurodegenerative diseases, such as Alzheimer's diseases.

The invention relates to a kit for rapidly detecting organophosphorus pesticide residues and an application method thereof. The kit comprises a C enzyme bottle, a T enzyme bottle, a C substrate reaction cup and a T substrate reaction cup, wherein the C enzyme bottle and the T enzyme bottle are sealed by using enzyme bottle sealing covers and are filled with an enzyme lyophilized three-enzyme mixing agent; the C substrate reaction cup and the T substrate reaction cup are provided with lyophilization and water-absorption cushions containing acetyl choline, luminol and dimethylbenzidine. The invention further relates to a method for applying the kit to rapidly detecting the organophosphorus pesticide residues. The kit takes acetylcholin esterase, choline oxidase and peroxidase as a catalysis system; a product obtained by hydrolyzing and oxidizing acetylcholine chloride and luminol have a chemiluminescence effect. A method for flexibly testing organophosphorus pesticides in agricultural products is established. The kit has the advantages of high detection speed, simple operation process, good stability and repeatability, no need of expensive instruments and the like, and is very suitable for carrying out field monitoring on the organophosphorus pesticides in farm markets.

The invention discloses a device and a method for detecting pesticide residue based on a multilayer paper microfluidic chip in the technical fields of microfluidic technology and pesticide residue. The method comprises the following steps: adding a to-be-detected sample into a cutting and stirring device, cutting and stirring to obtain sample mixed liquid, adding distilled water into a water-absorbing pad at the left sampling opening dropwise, enabling the liquid to arrive at a lime heating area through a paper channel, heating a paper chip in the lime heating area, adding the sample mixed liquid into the water-absorbing pad at the left sampling opening dropwise, combining the sample mixed liquid and an acetyl choline fixture after passing through a hydrophobic channel, producing an inhibition reaction on acetylcholin esterase through a left paper channel, developing, detecting a developing solution by using a photoelectric detection device, and processing a detection signal by a controller to obtain the concentration of pesticide. According to the method and the device, sample introduction, heating, reaction and developing are integrated, the detection cost is low, the detection speed is high and the accuracy is high.

There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.

The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.

The invention discloses a polypeptide combination method for wrinkle reduction. Through one or more polypeptides, the fusion of vesicles and a cell membrane is inhibited so that release of acetyl choline is inhibited. The polypeptide combination method utilizes a wrinkle reduction polypeptide composition with a mass concentration of 0.001% to 5%, a humectant with a mass concentration of 0.001%-10%, an antibacterial stabilizer with a mass concentration of 0.001%-2%, a preservative with a mass concentration of 0.001%-2% and a pH adjuster. The wrinkle reduction polypeptide composition comprises one or more of acetyl hexapeptide-8, palmitoyl pentapeptide-4, venom-like peptide and copper tripeptide-1 and the balance of deionized water and has a mass concentration of 0.001%-5%. According to thewrinkle production mechanism and different polypeptide action targets, the invention provides the wrinkle reduction polypeptide composition.

The invention provides a preparation method and application of a cobaltosic oxide / graphene aerogel composite material. The cobaltosic oxide / graphene aerogel composite material can be used in the field of colorimetric method based detection, especially used for colorimetric method based acetyl choline detection. A water solution prepared by oxidized graphene and soluble cobalt salt is transferred into a cylindrical container, then the cylindrical container is moved into a polytetrafluoroethylene hydrothermal kettle to perform constant-temperature thermal reaction, a drying technology is adopted to prepare the cobaltosic oxide / graphene aerogel composite material, and the preparation method is simple. The prepared cobaltosic oxide / graphene aerogel composite material has excellent conductivity, good electronic transmission performance and large localization range, and catalytic effect is remarkably improved. The prepared cobaltosic oxide / graphene aerogel composite material is creatively applied to colorimetric method based acetyl choline detection, operation is simple and convenient, the used instruments are low in price, and the research field of graphene aerogel based materials is widened.

The present invention relates a tacrine-8-hydroxyl(amine)quinoline derivative and applications thereof, and belongs to the technical field of biological medicines. The derivative comprises a compound of a formula I and a pharmaceutically acceptable salt thereof. A preparation method thereof comprises the step of: performing reductive amination and deprotection on the compounds Id and Ii and an intermediate In / In' to obtain a compound I, wherein the compound I can react in an alcohol solution to produce a salt. Pharmacological tests verify that the compound has the activity against Alzheimer's disease and can inhibit acetylcholinesterase and butyrylcholinesterase activity, and meanwhile can inhibit self-polymerization of the beta-amyloid protein, and has a certain chelating effect on metal ions, particularly Cu<2+> and Zn<2+>, so that the hydrolysis of the acetylcholinesterase and the self-polymerization of the beta-amyloid protein are retarded, the effect of the acetylcholinesterase on synapses is improved, and the metal ions in the brain is regulated, and therefore the compound is effective for treating Alzheimer's disease.

Medical data provided by a physiological parameter sensor is used for management of the patient's medical condition. Analytes that may be monitored and managed include, but are not limited to, acetyl choline, amylase, bilirubin, cholesterol, chorionic gonadotropin, creatine kinase (e.g., CK-MB), creatine, glucose, glutamine, growth hormones, hormones, ketones, lactate, oxygen, peroxide, prostate-specific antigen, prothrombin, thyroid stimulating hormone, and troponin.

The invention discloses a method for detecting the concentration of acetylcholin esterase. The method comprises the following steps that: S1: preparing carbon quantum dots, and preparing the carbon quantum dots into carbon quantum dot solution; S2: preparing acetylcholin esterase standard solutions of different concentrations, and independently adding acetyl choline solution, choline oxidase solution, horseradish peroxidase solution and o-phenylenediamine solution into the carbon quantum dot solution, and obtaining a mixed liquid system; S3: independently adding the carbon quantum dot solutioninto the mixed liquid system to obtain a standard sample system; S4: independently detecting the fluorescence intensities I442 and I573 of the standard sample system on the positions of 442nm and 573nm, and establishing a linear relational expression between I573 / I442 and the concentration of the acetylcholin esterase; and S5: preparing the to-be-detected solution of the acetylcholin esterase, and referring to S2, S3 and S4 to obtain the concentration of the acetylcholin esterase in the to-be-detected solution of the acetylcholin esterase. The method has the advantages of high-sensitivity identification and the like of the acetylcholin esterase in the sample.

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 to the 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 relates to a medical composition having the effect of restraining acetyl cholinesterase, as well as a synthetic method and an application of the medical composition, in particular to a carbamate compound with a general formula (I), wherein the definition of a symbol A is as shown in the description. The invention discloses the structure of the carbamate compound, the synthetic method thereof and the application of the carbamate compound in restraining the in vitro activity of acetyl cholinesterase, and an insecticide and a new medicine for treating Alzheimer's diseases can be further developed from the carbamate compound.

The present invention relates to pharmaceutical technology, and is especially (+)-Meptazinol diligand derivative as shown in the structural general expression and / or its salt and the preparation process. The present invention modifies the structure of (+)-Meptazinol through eliminating its N-methyl radical and connecting two N's on the seven-membered rings of two (+)-N-nor Meptazinol with hydrocarbon chains in different lengths to obtain the (+)-Meptazinol diligand derivative. The pharmacological experiment shows that the (+)-Meptazinol diligand derivative possesses analgesic activity of different degree.

Compounds represented by general formula (I), their stereoisomers, tautomers, derivatives, prodrugs or pharmaceutically acceptable salts, and their preparation methods or uses for the manufacture of a medicament of analgesics. In which R1 is selected from H, substituted or unsubstituted phenyl, or substituted or unsubstituted heteroaryl; A is bond, or saturated or unsaturated straight-chain or branched-chain hydrocarbon radical; R2, R3 are each independently hydrogen or methyl, which linked with any position of spirocyclo-structure; n and m are each independently integer between 0-2, do not represent 0 at the same time; B and D are each independently C1-C3 straight-chain or branched-chain alkylene; Y is selected from —CHR4—, O, S, —S(O)—, —SO2—, —NR4— and substituted or unsubstituted phenylene, in which R4 represents H, C1-C6 saturated or unsaturated alkyl, methyl or ethyl substituted by substituted or unsubstituted aryl or heteroaryl; and X− is pharmaceutical acceptable organic or inorganic anion. These compounds can be used as muscarine receptor (M-receptor) and / or nicotine acetylcholine receptor (N-receptor) agonist or antagonist. These compounds have good analgesic effect without side effect such as addiction.

The present invention relates to a pharmaceutical composition comprising propiverine, trospium or glycopyrrolate; and a non-anticholinergic antiemetic agent. It is also related to a pharmaceutical composition comprising a high dose of solifenacin or a pharmaceutically acceptable salts thereof; and a non-anticholinergic antiemetic agent. Pharmaceutical compositions containing high dose of nsPAChA for use for increasing the AChEI blood concentrations and for combating neurodegeneration are also described. The invention also relates to a method for inducing neuroprotection and combating neurodegeneration in a patient suffering from Alzheimer type dementia as well as to a method for increasing the blood levels of an acetyl choline esterase inhibitor (AChEI) in a human subject treated with an AChEI dose.

The invention discloses effervescent tablets for preventing and treating rice grubs and a preparation method thereof. The effervescent tablets are prepared from, by weight, 30-40 parts of pink plumepoppy herb, 20-32 parts of datura seeds, 18-30 parts of leaves of nerium odorum, 8-20 parts of radix sophorae subprostratae, 8-16 parts of acid source, 8-16 parts of alkali source, 2-4 parts of lubricating agent, 50-60 parts of filler, 4-8 parts of adhesive, 2-4 parts of disintegrating agent and 1-3 parts of wetting agent. According to the effervescent tablets for preventing and treating the rice grubs, pink plumepoppy herb, datura seeds and leaves of nerium odorum with neurotoxicity on the rice field grubs are added firstly, nervous excitation of the grubs is caused, acetyl choline reacting is interdicted, convulsion and spasm happen, a stomach poisoning effect is achieved on the grubs, and the intestinal tissue and other digestion and absorption organs are damaged; on this basis, radix sophorae subprostratae with a broad-spectrum antibacterial function is added, the two substances are compounded and added and achieve a synergistic effect, and the rice grubs can be effectively killed.

The present invention relates to novel heteroaryl diazacycloalkane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

The invention relates to the field of nano catalysis, environment protection and analytical chemistry, in particular to a test strip for rapidly detecting pesticides. Ferroferric oxide nanoparticles with pseudo peroxidase activity are in-situ generated on the test strip, and acetylcholin esterase and choline oxidase are modified on the test strip; when organophosphorus pesticides exist, the activity of the acetylcholin esterase is irreversibly inhibited to ensure that the amount of choline generated by acetyl choline hydrolysis is reduced, so that the hydrogen peroxide generated through cascade reaction is decreased and the developing of chromogenic substrates becomes light. Through a chromatography phenomenon of test paper, interferences of other substances in samples can be eliminated. Though mobile phone photographing and mobile phone software analysis, convenient quantitative detection for acetyl choline can be realized. The test strip can be used for the fields of pesticide residual analysis, biological medicine, environment monitor and the like.

The invention provides a method for detecting the acetyl choline content in peripheral blood mononuclear cells. The method provided by the invention lays a foundation for accurately detecting the ACh (acetyl choline) content by separating an ACh ingredient from a sample to be detected by adopting a UPLC (ultra performance liquid chromatography) technology. According to the technical scheme, an HILIC (hydrophilic interaction chromatography) column is found to be more suitable for separation of a polar compound by adopting experimental measures, can be used for effectively separating ACh from iso-ACh, and has a better separation effect on Cho. On this basis, chromatographic conditions and internal standard substance categories are further designed, and d9-ACh of isotope is taken as national standard substances of ACh and iso-ACh at the same time to furthest reduce the analysis error caused by sample damage and effectively ensure the accuracy of a measurement result. According to the method provided by the invention, on the basis of effectively separating ACh by using the UPLC, ACh signal detection is performed by a liquid chromatography-mass spectrometry system, and the ACh is accurately quantified by optimizing mass spectrometer conditions with a stable and accurate result and favorable linearity and sensitivity; meanwhile, the method has relatively low detection limit and relatively high recovery rate and also has a broad application prospect.

The invention provides a detection method for obtaining rat sinkaline signals through Proton MR spectroscopy (<1>H MRS) and then indirectly reflecting the content of acetylcholines in a rat. The method compares the content relationship of total sinkaline and acetylcholines in a sea horse area, a striaturn area, a frontal cortex area and a somatic cortex area of the normal rat; the contents of the total sinkaline and the acetylcholines of the rat in the four brain areas have obvious relativity through double variant and linear regression analysis. As shown by the result, the rat sinkaline signals obtained through the Proton MR spectroscopy are used as the predicated value of the content of the acetylcholines in the rat, which has statistic significance. Simultaneously, loss of the acetylcholines is a very important neuropathological variation of presenile dementia, thereby the method is hopeful to be applied to noninvasive early clinical diagnosis of the presenile dementia.

The invention belongs to the field of biochemistry and molecular biology, and relates to an alpha-conotoxin peptide TxIC / Txd1 and a medicinal composition and application thereof. The alpha-conotoxin peptide can specifically block an acetyl choline receptor (nAChRs, such as alpha3beta4 nAChR (nicotinic acetylcholine receptor)), has curative activity to habituation, neuralgia, Parkinsonism, dementia, schizophrenia, depression, cancers, fear and the like, and has a good application prospect on the aspect of preparation of smoking cessation, drug treatment and pain relieving medicaments, medicaments relevant to the treatment of mental diseases and cancers, neuroscience tool medicaments and the like.

The invention discloses application of berberine or other pharmaceutically acceptable salts in preparing a M3 receptor selective inhibitor medicine. The medicine is used for treating acute pancreatitis, lung cancers and colon cancers, self-immunity sialadenitis, asthma, respiratory tract inflammation, lung diseases and cardiovascular diseases, relieving panic, or treating excessive activity of bladders, and is used for inhibiting the enhancing of Ca<2+> signals in pancreatic acinar cells caused by M3 receptor-mediated acetyl choline and L-arginine.

The invention discloses an application of pentapeptide KLPGF in inhibiting AChE activity. The amino acid sequence of AChE inhibiting peptide is Lys-Leu-Ro-Gly-Phe (KLPGF). The KLPGF activity peptide can effectively inhibit the AChE activity, improve the level of brain neurotransmitter acetyl choline and play the effect of preventing senile dementia. The AChE inhibiting peptide is simple in structure, safe and free from toxicity; the AChE inhibiting property is strong and can be used for developing healthcare food or drug for assisting to release or treat the senile dementia.

The invention provides a biological sensor, a preparation method, application in detection of acetylcholin esterase, and a method for detecting an organophosphorus pesticide. The method is characterized in that acetyl choline has mimic enzyme to catalyze and oxidize TMB (3,3',5,5'-tetramethylbenzidine) to discolor, and can be decomposed and deactivated by the acetylcholin esterase, but the decomposing of hydrogen peroxide cannot be catalyzed, so that the TMB solution cannot generate color developing reaction; a linear relationship of absorbance and acetylcholin esterase is built, and the acetylcholin esterase is quantitatively detected; furthermore, the organophosphorus pesticide can effectively inhibit the activity of the acetylcholin esterase, the acetylcholin esterase is deactivated, the deactivated acetylcholin esterase cannot decompose the acetyl choline, and the TMB solution is promoted to generate the color developing reaction, thereby detecting the organophosphorus pesticide.

The invention provides application of acetyl choline in improving accumulation of microalgae polyunsaturated fatty acids and alpha-linolenic acid. The invention discloses application of acetyl choline in improving accumulation of microalgae polyunsaturated fatty acids and alpha-linolenic acid, and belongs to the technical field of microalgae organisms. The application comprises the following specific operation steps: (1) adding neurotransmitter acetyl choline in different concentrations at different growth periods of the microalgae; and (2) analyzing influences of the neurotransmitter acetyl choline in different concentrations, which are added at different periods, on polyunsaturated fatty acids and alpha-linolenic acid in microalgae grease. The invention discloses a method of increasing the content of the polyunsaturated fatty acids and alpha-linolenic acid in the microalgae grease in a growth process of the microalgae for the first time, so that a new thought is provided for promoting the accumulation of microalgae polyunsaturated fatty acids and alpha-linolenic acid in the microalgae grease by using a chemical method.