67 results about "Acetylcholine pathway" patented technology

A sensor is disclosed, for implantation within a blood vessel to monitor a substance in or property of blood. In one embodiment, the sensor detects nitric oxide or a nitric oxide metabolite. In another embodiment, other substances such as glutamate, aspartate, arginine, citrulline, acetylcholine, calcium, potassium, or dopamine are monitored. The sensor may be attached to a support structure such as a stent, guidewire, or catheter. In a further embodiment, a catheter is disclosed that extracts patient fluid to a sensor outside the body for monitoring a substance or property of the patient fluid. Methods are also disclosed.

This invention describes the administration of multiple therapeutic agents with insulin in conjunction with bexarotene, ketamine, monoclonal antibodies Etanercept, IGF-1, and acetylcholine esterase inhibitors physostigmine, for treatment of Alzheimer's disease and other neurodegenerative diseases. Insulin, improves memory; also augments and amplifies the effects of the adjuvant therapeutic agents (paracrine and intracrine effects) and consequently reduces the β amyloid, its soluble precursors, prevents damage to the neuronal skeletal network (taupathy), and blocks glutamate excitotoxicity, reduces brain inflammation, prevents apoptosis, and increases the acetylcholine levels in the neurons and synapses; by using a combination of insulin, bexarotene, ketamine, Etanercept, IGF-1, and physostigmine therapeutic agents. The results are achieved by using the specially designed Iontophoresis incorporated olfactory mucosal delivery (ORE) catheter device located at the olfactory nerves, sphenoid sinus, and adjacent structures described here, to transport the large molecules of therapeutic agents to treat AD delivered to the CNS bypassing BBB from ORE.

Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy.The invention particularly relates to a potent positive allosteric modulator of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.

A composition and a method for improving neuromuscular facilitation, also known as “muscle memory,” and enhancing cognitive functions, such as memory and mental focus. The dietary supplement, and the method for the administration thereof, increases acetylcholine levels, which improves neuromuscular facilitation. In various embodiments, factors other than increasing acetylcholine levels within the body further contribute to the overall effect of the dietary supplement composition. In a preferred embodiment, the invention is a composition, and a method for the administration thereof, comprising effective amounts of choline, dimethylaminoethanol, cytidine 5′-diphosphocholine, turmeric extract, decaffeinated green tea extract, vitamin B1, vitamin B5, vitamin B6, vitamin B12, folic acid, dimethylglycine, huperzine A, Griffonia simplicifolia extract, and 1-phenylalanine, magnesium stearate, and silicon dioxide.

The present invention concerns methods for treating or preventing neurological disorders characterized by dysfunction of nicotine acetylcholine receptors by co-administration of metanicotine and at least one compound which exhibits antagonist activity, or both agonistic and antagonist activity, toward one or more nicotinic acetylcholine receptor subtypes. The subject invention, in another aspect, pertains to pharmaceutical compositions containing metanicotine and at least one compound which exhibits antagonistic activity, or both agonistic and antagonistic activity, toward one or more nicotinic acetylcholine receptor subtypes.

Carbamoyl esters inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. In one embodiment, the carbamoyl ester has the following structure: Formula (I) wherein A is selected from the group consisting of an unsubstituted aryl, a substituted aryl, an unsubstituted heteroaryl and a substituted heteroaryl. The carbamoyl esters are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the carbamoyl esters can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

The present invention provides methods for assessing the activity of topically administered chemodenervating agents. In some embodiments, methods for assessing the activity of topically administered chemodenervating agents involve determining the extent of inhibition of acetylcholine release near the site of administration. In some embodiments, methods for assessing activity of topically administered chemodenervating agents involve observing a reflex motion of a limb of a subject.

A quick residual detecting method for conventional pesticide features that the acetylcholine esterase from the liver of white rats is used as the source of the enzyme. The acetylcholine is used as the substrate. Under the action of acetylcholine esterase, the substrate is hydrolyzed so as to generate the sulfocholine and DTNB. The peak of the maximum absorption in the color reaction is at 412 nm.With concentration of enzyme being fixed, comparing OD412 value of the pesticide in different concentrations establishes the standard curvature. With being dipped and extracted, the sample to be measured is tested so as to obtain the value of OD412. Base on the value of OD412 of the sample to be measured, the residual concentration and the depression rate of the pesticide in the sample to be measured in determined.

Compounds that inhibit cholinesterase activity and, upon hydrolysis release a pharmacologically active agent. The compounds of the invention are employed in methods to treat an individual. The pharmacologically active agent obtained by hydrolysis of the compound can treat, for example, a nervous system condition, a cholinergic deficiency and conditions or diseases associated with a deficiency in a pharmacologically active agent, such as acetylcholine.

An alkyl ether derivative represented by the formula: wherein R1, R2, R3, R4, m and n are as defined in the specification, or salts thereof exhibits synergistically improved anti-hypoxic activity when combined with a compound having an acetylcholine esterase inhibitory activity. Therefore, the combination according to the present invention is useful as a method for improving cerebral function. Further, a pharmaceutical composition containing the compound relating to the combination according to the present invention is useful for treatment and prevention of dysfunction of cerebral acetylcholine neurons in the sequelae of cerebrovascular dementia, senile dementia, Alzheimer's disease and ischemic cerebral lesion and in the cerebral apoplexy or the memory impairment caused by selective neuronal death.

The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1 -azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the α7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.

The invention provides a PVC (Poly Vinyl Chloride) foaming simulated wood floor comprising the following raw materials in parts by weight: 100-150 parts of PVC powder, 100-150 parts of straw powder, 20-35 parts of light calcium carbonate, 0.5-1.0 part of a foaming agent, 2.0-5.0 parts of a foaming modifier, 0.5-1.0 part of a lubricating agent, and 5.0-5.5 parts of a stabilizer, wherein the foaming agent is an ACH (acetylcholine) composite foaming agent; the foaming modifier is an acrylic polymer; the lubricating agent is calcium stearate or oxidized polyethlene wax; and the stabilizer is zinc laurate or zinc stearate or epoxidized soybean oil. The PVC foaming simulated wood floor provided by the invention has the advantages of strong solid wood appearance, light weight, water proofing, good abrasion resistance and wide application prospect.

The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the α7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.

The invention discloses a multizone multifunctional nerve dual-mode detection microelectrode array chip and a preparation method thereof. The chip comprises an insulation substrate, multiple contacts, multiple strip leads and multiple microelectrode arrays. The invention also provides a preparation method of the multizone multifunctional nerve dual-mode detection microelectrode array chip. According to the technical scheme, not only the decorated electrode surface can be employed for culturing nerve cells for synchronously detecting electrophysiological signals and electrochemical signals of neurotransmitters such as acetylcholine and the like of four-group nerve cells under different experiment parameters in real time, but also the four functional zones are employed for decorating different sensitive materials and further for culturing nerve cells for detecting nerve electrophysiological signals in real time and further for comparing the characteristics of different decoration materials. The chip provided by the invention integrates multiple functions, is simple in technological preparation and convenient to use, and is suitable for laboratories to develop research related to nerve cell culture and multi-parameter nerve dual-mode signal detection of nerve cells.

The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I).The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.

An alkyl ether derivative represented by the formula: wherein R1, R2, R3, R4, m and n are as defined in the specification, or salts thereof exhibits synergistically improved anti-hypoxic activity when combined with a compound having an acetylcholine esterase inhibitory activity. Therefore, the combination according to the present invention is useful as a method for improving cerebral function. Further, a pharmaceutical composition containing the compound relating to the combination according to the present invention is useful for treatment and prevention of dysfunction of cerebral acetylcholine neurons in the sequelae of cerebrovascular dementia, senile dementia, Alzheimer's disease and ischemic cerebral lesion and in the cerebral apoplexy or the memory impairment caused by selective neuronal death.

Described herein is a combination comprising at least one 5-HT4 receptor agonist and at least one phosphodiesterase 4 (PDE4) inhibitor, and methods and uses thereof in the prevention and / or treatment of one or more disorders in which an increased acetylcholine release is desired; for example in the prevention and / or treatment of gastrointestinal disorders, urinary disorders, and / or respiratory disorders.

The biological catalyst as one kind of composite biological functional material includes two reagent components packed separately, the reagent A consists of metal ion 0.5-1 wt%, 2D resin 7-9 wt%, titania 66.3-71.7 wt% and zinc oxide 1.3-13.3 wt%; and the reagent B consists of L-serine 0.2-0.5 wt%, cystine 0.2-0.5 wt%, acetylcholine 0.5-0.7 wt% and hinokitiol 12-16 wt%. It can distinguish pathogenetic microbes fast and accurately and kill pathogenetic microbes only, and has no irritation to human body, no side effect, no influence on human body immunity, high physical and chemical stability, wash resistance, and no influence on the characteristics and indexes of fabric.

The invention discloses a wear-resisting coating. The wear-resisting coating comprises the following raw materials in parts by weight: 20-30 parts of vinyl triisopropoxysilane, 3-5 parts of silicon dioxide aerogel, 15-20 parts of trioxane, 5-9 parts of water, 3-7 parts of acetic anhydride, 10-15 parts of acetylcholine, 0.1-0.3 part of polyoxyethylene anhydro-sorbit monoglyceride, 10-15 parts of crystallizing silicon oxide, and 7-13 parts of graphite powder, wherein the porosity of the silicon dioxide aerogel is 75-79%, and the weight ratio of silicon dioxide aerogel to vinyl triisopropoxysilane is 1:(5-7). The wear-resisting coating can improve the degree of crosslinking of a coating and enhance the resistance to scratching, and has low cost.

A composition of matter for an analgesia and its method of use is disclosed. The method of use is for the treatment of chronic pain, especially to the treatment of heretofore intractable pain as associated with advanced cancer. The pain associated with neurological conditions, rheumatoid arthritis, viral infections and lesions is also contemplated. The method includes administering to a host an alpha-neurotoxin that is characterized by its ability to blocking of the action of acetylcholine at nicotinic acetylcholine receptors.

The present invention relates to the use of a medicinal substance capable of enhancing or disinhibiting the actions of acetylcholine, and provides a pharmaceutical composition for treating drug dependence comprising said substance as an active ingredient, and a method of treating drug dependence using the same.

The cobra neurotoxin is capable of binding to nicotinic acetylcholine receptors after nerve synapses to block neuronal caudal ion flow to realize analgesic effect, however, the product on the market takes 2 hours to be effective and the curative effect is unstable, which cannot meet clinical requirement. The neurotoxins need to pass a blood cerebral barrier in the brain to play an analgesic effect, and the product on the market has no clear components, including various molecular weight proteins, so the speed for permeating the blood cerebral barrier is slow; and at the same time, affinity with the nicotinic acetylcholine receptors is also inconsistent. The application screens a group of neurotoxin molecular monomers having high affinity with the nicotinic acetylcholine receptor, can quickly pass the blood cerebral barrier, and has analgesic effect and stable therapeutic effect in 30 minutes. The neurotoxin molecular monomer overcomes the defects that a mixture cannot specify which neurotoxin is present, the protein primary structure is not existed, the quality cannot be precisely controlled; according to the invention, the quality is controlled, clinical safety and effectiveness are better guaranteed.

This invention provides a method for treating or preventing human atrial arrhythmia (fibrillation) using the leading flavone compound acacetin, and its derivatives and analogues that inhibit the ultra-rapidly-activating delayed rectifier potassium current (IKur or IKsus), transient outward potassium (Ito), and acetylcholine-activated potassium current (IK.ACh).

The invention relates to the field of compound fertilizers, and in particular relates to a catechol-containing polyurethane coated slow release compound fertilizer which comprises the following raw materials by weight: 10-15 parts of 1250-2000 mesh diatomite, 6-9 parts of bean curd wastewater, 12-15 parts of phosphorus pentoxide, 6-8 parts of sodium poly aspartate, 20-22 parts of rotten porch fertilizer,, 10-12 parts of rotten Chinese medicine residue, 15-18 parts of ammonium hydrogen carbonate, 2-4 parts of ferrous sulfate, 12-15 parts of phosphogypsum, 2-3 parts of methionine, 16-18 parts of rice chaff, 2-4 parts of catechol, 1-3 parts of acetylcholine, 0.1-0.2 part of sodium nitrophenolate, 20-25 parts of palm oil modified waterborne polyurethane emulsion, 3-5 parts of colloidal lithium magnesium silicate and 4-5 parts of auxiliaries; the catechol-containing polyurethane coated slow release compound fertilizer is extensive in raw material sources, multi-nutrient, and nutrient-rich, nutrients are doubly coated by the diatomite and a slow release coating agent in the production process, the fertilizer efficiency is long-lasting, crop resistance is strong, incidence of pests diseases and insect pests is low, and yield and quality are promoted.

The invention discloses an environment-friendly coating for a steel ring wheel. The environment-friendly coating is prepared from the following components: a polyurethane emulsion, butyl acetate, vinyl silicone oil, nanometer titania, attapulgite, mica powder, acetylcholine, water, aluminum borate whisker, menthyl acetate, vegetable gelatin, a plant extract and a coalescing agent. After the coating is formed into a film, the film is high in hardness, good in abrasion resistance, short in hard drying time, good in abrasion resistance and fracture resistance, excellent in abrasion resistance and good in adhesive force. The prepared coating is good in stability, has better stability after being used for a long time, and is low in possibility of cracking, and fine cracks are low in possibility of expanding and better in repairability, so that the intrinsic strength and the stability of the coating are greatly improved, and the life span is greatly prolonged. According to the coating, through synergetic cooperation function of the components, the life span of the coating film formed by the coating is greatly prolonged, and is increased by 400% as compared with that of the coating film formed by the common polyurethane emulsion coating.

The present invention relates to an alpha7 nicotinic acetylcholine receptor ligand and a preparation method thereof. The ligand includes an agonist and an imaging agent, the agonist is a 1,4-diazabicyclo [3.2.2] nonane-benzo heterocyclic derivative, and the imaging agent is 125I and 18F-trifluoromethyl marker. The derivatives both have good brain uptake, the absorption values in different regions of the brain are basally consistent with the distribution of alpha7nAChR receptors, the uptake of the derives is highest in hippocampus, thalamus, cortex and other regions where the alpha7nAChR receptors targetedly distribute, and the derives can be blocked by known alpha7nAChR ligands but can not be blocked by alpha4beta2 medicine. Therefore, the 1,4-diazabicyclo [3.2.2] nonane-benzo heterocyclic derivative and the 125I and 18F-trifluoromethyl marker are potential agonist and imaging agent for alpha7 nicotinic acetylcholine receptors.

The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).

The invention relates to an acetylcholine detection kit based on the protein-inorganic hybrid nanoflower and a preparation method thereof and belongs to the technical field of a biosensor. The kit isloaded with the protein-inorganic hybrid nanoflower, acetylcholinesterase, choline oxidase and color developing agent. Through the acetylcholinesterase, the acetylcholine can be catalyzed to produce choline, the choline is further oxidized by the choline oxidase to produce hydrogen peroxide, and the formed hydrogen peroxide is catalytically oxidized by a hydroxyl group to generate a hydroxyl radical to further develop the color developing agent. The kit is advantaged in that the acetylcholine can be rapidly detected by the kit, a direct quantification tool is provided for identification of theacetylcholine, simple and convenient operation, high sensitivity and low cost are realized, the portable on-site test kit is provided for immediate testing of the activity of the acetylcholine, and the needs of frequent screening and diagnostic tracking are met.