1007 results about "Acetylcholine" 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.

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 relates to insecticidal mixtures of spinosyns and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests.

A device and associated method for providing vestibular stimulation to an individual includes active elements positioned on or proximate an ear insert. The active elements include but are not limited to at least one electrode, at least one thermometer, and at least one thermoelectric transducer. The device includes a computerized control module regulating the active elements. The device incorporates an ear insert that allows the active elements to engage the individual's ear canal and therefore access the individual's vestibular system. Vestibular stimulation applied to the individual is customized for directly stimulating desired regions of the brain for therapeutic or diagnostic purposes. In a preferred embodiment, the device provides vestibular stimulation sufficient to promote physiological changes in the individual, the changes selected from the group consisting of circadian temperature cycle time shifts, ascorbic acid production, serotonin production, acetylcholine production, histamine production, and heat shock protein production.

There is provided a method of inducing differentiation of bone marrow stromal cells to neural cells or skeletal muscle cells by introduction of a Notch gene. Specifically, the invention provides a method of inducing differentiation of bone marrow stromal cells to neural cells or skeletal muscle cells in vitro, which method comprises introducing a Notch gene and / or a Notch signaling related gene into the cells, wherein the finally obtained differentiated cells are the result of cell division of the bone marrow stromal cells into which the Notch gene and / or Notch signaling related gene have been introduced. The invention also provides a method of inducing further differentiation of the differentiation-induced neural cells to dopaminergic neurons or acetylcholinergic neurons. The invention yet further provides a treatment method for neurodegenerative and skeletal muscle degenerative diseases which employs neural precursor cells, neural cells or skeletal muscle cells produced by the method of the invention.

There is provided a method of inducing differentiation of bone marrow stromal cells to neural cells or skeletal muscle cells by introduction of a Notch gene. Specifically, the invention provides a method of inducing differentiation of bone marrow stromal cells to neural cells or skeletal muscle cells in vitro, which method comprises introducing a Notch gene and / or a Notch signaling related gene into the cells, wherein the finally obtained differentiated cells are the result of cell division of the bone marrow stromal cells into which the Notch gene and / or Notch signaling related gene have been introduced. The invention also provides a method of inducing further differentiation of the differentiation-induced neural cells to dopaminergic neurons or acetylcholinergic neurons. The invention yet further provides a treatment method for neurodegenerative and skeletal muscle degenerative diseases which employs neural precursor cells, neural cells or skeletal muscle cells produced by the method of the invention.

RNA interference is provided for inhibition of ocular hypertension target mRNA expression for lowering elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. Ocular hypertension targets include carbonic anhydrase II, IV, and XII; β1- and β2 adrenergic receptors; acetylcholinesterase; Na+ / K+-ATPase; and Na—K-2Cl cotransporter. Ocular hypertension is treated by administering interfering RNAs of the present invention.

Tobacco products comprising smokeless tobacco products and active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel are disclosed. Nicotine replacement therapies comprising active ingredients, including those that antagonize nicotinic acetylcholine receptors, the TRPV1 channel, and / or the TRPA1 channel. The active ingredient may reduce or eliminate sensory irritation arising due to use of the product. Analgesic compositions comprising active ingredients. Methods of reducing taste and sensory irritation by employing an active ingredient.

Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and / or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Devices, systems and methods are disclosed for treating bronchial constriction related to asthma, anaphylaxis, chronic obstructive pulmonary disease (COPD), exercise-induced bronchospasm and post-operative bronchospasm. The treatment comprises transmitting impulses of energy non-invasively to selected nerve fibers that activate neural pathways to reduce the release of acetycholine from airway-related vagal preganglionic neurons within the brain of the patient. The transmitted energy impulses, comprising magnetic and / or electrical energy, stimulate the selected nerve fibers to produce the bronchodilation.

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 conotoxin peptides that are analogs of the α-contoxin peptide RgIA. These conotoxin peptides block the α9α10 subtype of the nicotinic acetylcholine receptor (nAChR) and can be used for treating pain, such as neuropathic pain and inflammatory pain, inflammatory disorders, such as rheumatic diseases, and in the treatment of breast cancer.

Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

The present invention provides a novel compound having an excellent acetylcholinesterase inhibitory effect. That is, it provides a 4-substituted piperidine compound fluoride represented by the following formula, a pharmaceutically acceptable salt thereof or hydrates thereof (provided that 1-benzyl-4-[(5,6-dimethoxy-2-fluoro-1-indanon)-2-yl]methylpiperidine, a pharmaceutically acceptable salt thereof and hydrates thereof are excluded).wherein R<1 >and R<2 >represent substituents.

The invention discloses preparation and application of total alkaloids extract and effective components in peganum plant seeds. The peganum plant (comprising harmel, multisectum peganum and peganum nigellastrum) seeds are heated, refluxed and extracted by ethanol, dissolved along with heat, acidulated by added 2 to 10 percent hydrochloric acid, and basified by ammonia water to separate out sediment; and the sediment is dried to obtain the total alkaloids extract mainly containing dehydrogenized peganine and peganine according to a proportion of between 0.18 to 1 and 4.30 to 1, wherein the content of the total alkaloids is more than 50 percent. The total alkaloids extract is separated by chromatography to obtain ten effective monomer components such as the dehydrogenized peganine, the peganine, and the like. Through thin layer chromatography and biological self-developing analysis, the total alkaloids extract and the effective monomer components thereof have the effect of resisting activity of acetylcholine esterase, and can be used for preparing medicament for resisting the activity of the acetylcholine esterase and medicament for treating neurodegenerative diseases.

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 device and associated method for providing vestibular stimulation to an individual includes active elements positioned on or proximate an ear insert. The active elements include but are not limited to at least one electrode, at least one thermometer, and at least one thermoelectric transducer. The device includes a computerized control module regulating the active elements. The device incorporates an ear insert that allows the active elements to engage the individual's ear canal and therefore access the individual's vestibular system. Vestibular stimulation applied to the individual is customized for directly stimulating desired regions of the brain for therapeutic or diagnostic purposes. In a preferred embodiment, the device provides vestibular stimulation sufficient to promote physiological changes in the individual, the changes selected from the group consisting of circadian temperature cycle time shifts, ascorbic acid production, serotonin production, acetylcholine production, histamine production, and heat shock protein production.

A sensor and method for detecting biological and chemical agents comprising metal interdigitized electrodes coated with hybrid polymer-based conducting film and an instrument for applying electrical voltage to the electrodes and registering the change in electrical current. The hybrid film also comprises indicator biomolecules encapsulated within the film or attached to it. The bioindicator molecules preferably comprise enzyme acetylcholinesterase. When these indicator biomolecules come in a contact with a pathogen, chemical and / or morphological changes occur in the film and electrical current flowing through the electrodes is modulated. The pathogen comprise inhibitors of enzymes, preferably organophosphates, thiophosphates or phosphonates. The change in current indicates the presence of a biological and chemical agent and is registered.

Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and / or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.

Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

Methods for treating an individual with a psychiatric order with a pharmacologic agent that enhances learning or conditioning in combination with a session of psychotherapy are provided. These methods of the invention encompass a variety of methods of psychotherapy, including exposure-based psychotherapy, cognitive psychotherapy, and psychodynamically oriented psychotherapy, and psychiatric orders including fear and anxiety disorders, addictive disorders including substance-abuse disorders, and mood disorders. The pharmacologic agents used for the methods of the present invention are ones that generally enhance learning or conditioning, including those that increase the level of norepinephrine in the brain, those that increase the level of acetylcholine in the brain, and those that enhance N-methyl-D-aspartate (NMDA) receptor transmission in the brain.

The invention provides a method of preventing, delaying, or reversing the progression of Alzheimer's disease by administering an Aβ42 lowering agent to a mammal under conditions in which levels of Aβ42 are selectively reduced, levels of Aβ38 are increased, and levels of Aβ40 are unchanged. The invention provides methods and materials for developing and identifying Aβ42 lowering agents. In addition, the invention provides methods for identifying agents that increase the risk of developing, or hasten progression of, Alzheimer's disease. The invention also provides compositions of Aβ42 lowering agents and antioxidants, Aβ42 lowering agents and non-selective secretase inhibitors, as well as Aβ42 lowering agents and acetylcholinesterase inhibitors. The invention also provides kits containing Aβ42 lowering agents, antioxidants, non-selective secretase inhibitors, and / or acetylcholinesterase inhibitors as well as instructions related to dose regimens for Aβ42 lowering agents, antioxidants, non-selective secretase inhibitors, and acetylcholinesterase inhibitors.

Muscarinic Acetylcholine receptor antagonists and methods of using them are provided.

This document provides methods and materials related to regulating inflammatory pathways. For example, compositions and kits containing two or more of an anticholinesterase compound, a choline compound, and a carnitine compound and methods for using the compositions and kits described herein to support acetylcholine function to regulate one or more inflammatory pathways are provided.

The invention relates to the imidazole derivatives as selective antagonistic substances against muscarinic acetylcholine and provides imidazole derivatives represented by a general formula (1) or (2) [wherein R1 is a phenyl group which may have substituent or thienyl group, R2 is a cyano group, a carboxyl group, CONR7R8 group (wherein R7 and R8 each independently represent hydrogen atom or lower alkyl group, or R7 and R8 may form a ring by alkylene chain which may contain hetero atom) or COOR9 group (wherein R9 is a lower alkyl group), R3 is a hydrogen atom or lower alkyl group, R4, R5 and R6 each independently represent hydrogen atom, lower alkyl group which may have substituent or cycloalkyl groups, or may form a condensed ring at the positions of R5 and R6 with benzene ring, R10 is a lower alkyl group or an aralkyl group which may have substituent, m is an integer from 1 to 6, and z is a halogen atom].

Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided.

The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and / or acting as cholinesterase inhibitors and / or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugs”, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.