109 results about "Cholinergic" patented technology

The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.

The present invention relates generally to compositions or formulations for transdermal or transmucosal administration of anticholinergic agents such as oxybutynin. The invention utilizes a novel delivery vehicle and is a substantially malodorous-free and irritation free transdermal formulation which is substantially free of long chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. A method is disclosed for treating a subject for urinary incontinence with these formulations while reducing the incidences of peak concentrations of drug and undesirable side effects associated with oral anticholinergics.

This invention relates to compounds, compositions, and methods useful for modulating cholinergic muscarinic receptor gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of cholinergic muscarinic receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of cholinergic muscarinic receptor genes, such as M3 muscarinic acetylcholine receptor or cholinergic receptor muscarinic 3 (CHRM3).

Compounds and methods are provided for the treatment of disease conditions in which modification of cholinergic, especially muscarinic m1, m4, or both m1 and m4, receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.

The invention belongs to the technical field of medicine, and discloses a preparation method of (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) four type chiral monomers of muscarine receptor antagonist racemic medicine glycopyrronium bromide. The method comprises the following steps: resolving racemic alpha-cyclopentylmandelic acid by a chemical resolution method by using L-Tyrosine methyl ester and (R)-alpha-phenylethylamine as resolution reagents to respectively prepare (S)-alpha-cyclopentylmandelic acid and (R)-alpha-cyclopentylmandelic acid; and carrying out esterification reaction to respectively obtain chiral intermediates (S)/(R)-alpha-cyclopentylmethyl mandelate. L/D-malic acid used as the raw material is subjected to four reaction steps, including condensation, carbonyl reduction, catalytic hydrogenation or transfer hydrogenation reduction debenzylation, and reduction alkylation or alkylogen alkylation, in a chiral synthesis mode to obtain another important chiral intermediate (S)/(R)-N-methyl-3-hydroxypyrrolidine. The chiral intermediate is subjected to ester exchange and quaterisation to respectively obtain the four (3S,2'S), (3S,2'R), (3R,2'R) and (3R,2'S) type glycopyrronium bromide chiral monomers. The result indicates that the (3R,2'S)-glycopyrronium bromide has the strongest cholinergic antagonistic action.

The present invention relates to novel alternative forms of human acetylcholinesterase (AChE) and nucleotide sequences encoding the same. The genes encoding the novel forms of human AChE have been identified in various malignant tumor cells. In a further aspect, the invention relates to a transgenic animal assay system for evaluating efficacy of drugs against cholinergic proteins, prior to or in the course of therapeutic treatment. Transgenic animals, preferably developing tadpole of Xenopus or mice which express human AChE, are used. The transgenic animal assay system is also useful for evaluating the toxicity of substances which potentially block human AChE (e.g. organophosphorous compounds).

The invention provides a method for preparing a 5,6,7,4'-tetrahydroxyflavone compound, which is characterized by comprising the following steps: taking breviscapinun as a raw material, and performing heating reflux reaction between the breviscapinun and alcohol under the catalysis of acid, namely adding 200 to 500 ml of alcohol substance and 1 to 3 ml of 4 to 5 percent acid into 12 to 20 g of the breviscapinun for the heating reflux reaction; and filtering a product, and drying to a constant weight to obtain 5,6,7,4'-tetrahydroxyflavone shown in a formula I. Experiments prove that the 5,6,7,4'-tetrahydroxyflavone shows obvious strengthening effect on acquisition, consolidation and representation of brain memory of a mice model of alzheimer disease, has obvious improving effect on learning memory of the mice model with memory loss caused by anisodine of an M-cholinergic inhibitor, and can obviously improve the recent memory and long-term memory capacities of mice. The experiments also prove that the 5,6,7,4'-tetrahydroxyflavone has the effect of treating arthritis, and also has good treating effects on diabetes mellitus and osteoporosis.

The invention discloses a series of 11-replaced oxoisoaporphine derivatives as well as a synthetic method and an application thereof. The synthetic method comprises the following steps: (1) carrying out ring closing reaction on 3-chlorophthalic anhydride and phenylethylamine as raw materials so as to construct a 10-Cl-1-azabenzanthrone parent body; (2) nitrating the parent body compound so as to obtain a 11-site nitrated product, and reducing the 11-site nitrated product so as to obtain 11-amino-10-chlorine-7H-dibenzoquinoline-7-ketone; and (3) reacting the 11-amino-10-chlorine-7H-dibenzoquinoline-7-ketone with an acyl chloride compound connected with piperidine so as to obtain a corresponding target product. Through study, the applicant finds that the series of derivatives have very strong inhibitory activity on acetylcholin esterase and are expected to be used for treating AD (Alzheimer Disease), cerebrovascular dementia and related diseases caused by cholinergic neurotransmitter reduction. The structural formula of the 11-replaced oxoisoaporphine derivatives is shown in descriptions.

Dry powder formulations for inhalation containing a combination of an anti-cholinergic, a long-acting beta₂-adrenoceptor agonist, and a corticosteroid are useful for the prevention and/or treatment of an inflammatory and/or obstructive airways disease.

Determination of anticholinergic M3 receptor and antibody is used to diagnose sicca syndrome. It has excellent sensitivity and specificity.

The invention relates to the technical field of NGS flavone medicine, specifically to an application of a Uighur drug nigella glandulifera preyn seed flavone in chronic obstructive pulmonary disease drug preparation. With the NGS flavones, a stable anti-chronic inflammation effect is provided for chronic bronchitis caused by chronic obstructive pulmonary diseases, lung bronchial spasm symptoms caused by chronic obstructive pulmonary diseases can be effectively improved, and generation of pulmonary bulla and emphysema can be prevented. The action mechanism relates to functions of lung bronchial smooth muscle M cholinergic receptor inhibition, and lung bronchial tissue inflammatory cell and inflammatory cytokine reduction, wherein the action mechanism is described in home and abroad researches at the first time.

A skin patch which improves symptoms of ashronesia, delusion and myasthenia caused by cholinergic deficit is composed of an antiseizing layer, a medicine storing layer and a back lining layer, wherein the medicine storing layer comprises medicine, dissolvent and pressure-sensitive adhesive. The invention is characterized in that the medicine is galantamin or hydrobromate thereof. The galantamin or hydrobromate thereof is 0.007mg-10mg/cm<2>, and the medication area is 2.5-70cm<2>. The pressure-sensitive adhesive is selected from polyisobutene pressure-sensitive adhesive, emulsion and dissolvent type acrylate. When the pressure-sensitive adhesive is polyisobutene, the medicine storing layer is composed of medicine, dissolvent, pressure-sensitive adhesive, thickening agent, anti-oxidant and transdermal promoter. When the pressure-sensitive adhesive is emulsion type acrylate, the medicine storing layer is composed of medicine, dissolvent, pressure-sensitive adhesive, thickening agent and concentrated ammonia liquor. When the pressure-sensitive adhesive is dissolvent type acrylate, the medicine storing layer is composed of medicine, dissolvent, and pressure-sensitive adhesive. The skin patch of the invention can effectively treat the symptoms of ashronesia, delusion and myasthenia caused by cholinergic deficit, increase the life quality of patient and alleviate the burden of kin and society.

The invention relates to the field of natural pharmaceutical chemistry and specifically provides a monoterpenyl bishydroxycoumarin compound, a pharmaceutical composition, a preparation method of the monoterpenyl bishydroxycoumarin compound, and application of the monoterpenyl bishydroxycoumarin compound and the pharmaceutical composition. The monoterpenyl bishydroxycoumarin compound has a structure as shown in a formula (I) which is described in the specification. In the formula, R1 to R6 and X1 to X4 are as defined in the specification. The monoterpenyl bishydroxycoumarin compound provided bythe invention can protect nerve cells from damage by inhibiting the activity of acetylcholin esterase, and has anti-inflammatory and antioxidant effects. Therefore, the compound can be used for preparing medicines for preventing and treating nervous system degenerative diseases such as senile dementia (also called Alzheimer's disease), cholinergic neurodegenerative change, learning and memory ability decline and the like.