297 results about "Acetylcholine esterase" patented technology

The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.

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.

This invention relates to a novel transdermal drug delivery system whereby Huperzine A ("Hup A"), a naturally occurred Acetylcholine esterase inhibitor traditionally used to alleviate memory problem, is formulated for transdermal administration suitable for the treatment of Alzheimer's Disease ("AD") to increase the efficacy and convenience for outpatient care of AD patients. A controlled-release skin patch designed for once-a-week application of Hup A is provided for easy AD medication according to the invention.

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.

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.

This invention belongs to pharmacy field, it relates optical pure mei pu ta fen and its preparation method and application. Racemation mei pu ta fen is splited by optical pure tartaric acid evolving object to get optical pure monomer, enantiomeric excess testing is done through capillary electrophoresis method, their e.e.valude are both excess 99 percent. Laevorotation and dextrorotation mei put a fen absolute configuration is decided by single crystal X-diffraction method as S and R. the R(+)mei pu ta fen has srong activity in analgesia activity testing, but S(-)mei pu ta fen has more stronger activity in acetylcholine esterase restrain activity testing, analgesic medicine and senile dementia medicine can be further prepared.

The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.

The invention discloses application of a near infrared-emission fluorescent probe in quick pesticide residue detection and belongs to the technical field of quick pesticide detection. The probe is based on rhoda-fluor fluorescence matrix and has specific activity on acetylcholine esterase AChE; by means of an enzyme inhibition detection principle, the probe can be applied to quick detection of organophosphorus pesticide and carbamate pesticide residues in food. The acetylcholine esterase AChE is extracted from duck blood; in an appropriate probe substrate range, enzyme activity and an inhibition rate can be represented by quantitatively detecting fluorescence intensity change of the probe. Four pesticide detection standard curves have small error, and R<2> is larger than 0.98; vegetable pesticide adding standard recovery most reaches 80 to 110%, so that the near infrared-emission fluorescent probe disclosed by the invention can be applied to quantitative, ppb-grade and quick detectionof organophosphorus and carbamate pesticide residues in the food.

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.

It is intended to provide a preventive/remedy for urinary disturbance containing a compound, which shows an acetylcholine esterase inhibitory activity but substantially has no butyrylcholine esterase inhibitory activity, showing no side effect and being safe and efficacious without inhibiting the urine collection function; a preventive/remedy for dry mouth induced by the administration of a remedy for urinary disturbance and a preventive or remedy for hyperactive bladder not accompanied by dry mouth; and a method of screening a substance preventing/treating urinary disturbance without inhibiting the urine collection function characterized by comprising measuring and comparing the acetylcholine esterase inhibitory activity and the butyrylcholine esterase inhibitory activity of a test compound.

A card for fast testing residual pesticide belongs to the technical field of biological engineering, and comprises two layers of plastic plates, wherein one of the plastic plates is provided with a sampling hole and an observation hole, one face of the plastic plate is provided with water-absorbing paper and an enzyme bar for fixing drosophila melanogaster acetylcholine esterase, the water-absorbing paper opposites the sampling hole, the enzyme bar opposites the observation hole, and the water-absorbing paper is connected with the enzyme bar. A base sheet for fixing indoxyl acetic ester is bonded on the other plastic plate at the position corresponding to the enzyme bar, and a baffle is arranged between the base sheet and the enzyme bar. When the sample and the indoxyl acetic ester in the enzyme bar pre-react, the baffle is drawn out to make the enzyme bar and the base sheet contact. The card for fast testing residual pesticide has the advantages of wide application range, delicate testing and fast and simple operation.

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.

The inventive aims to overcome the defects of the conventional enzyme inhibition-type biosensor and provides a visual identification method for detecting a micro-trace organophosphorus pesticide. When the detection method is adopted to detect the organophosphorus pesticide, on one hand, an adopted AChE liquid (Acetylcholine Esterase) is not subjected to solidification treatment, so that the highest activity of the AChE liquid is kept, and the detection sensitivity is improved; on the other hand, the extraction and recovery rate of the organophosphorus pesticide in a sample to be detected is improved through an adopted extracting solution, so that the detection sensitivity is improved to 0.01 ng/L. The detection method can be extensively applied to the detection of micro-trace organophosphorus pesticide residue in grains, vegetables, fruits and other agricultural products as well as the environment, and can also be used in the safety evaluation of agricultural products and the environment, the pollution condition monitoring of the organophosphorus pesticide, and the like.

The invention discloses a 3-aminoalkaneacylamino-rutaecarpine and 3- aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative and a synthetic method and an appliance thereof. As shown in experiments, the 3-aminoalkaneacylamino-rutaecarpine and 3-aminoalkaneacylamino-7,8-dehydrorutaecarpine derivative of the invention has strong inhibition perforance on acetylcholine esterase and good inhibition selectivity and the inhibition ability to acetylcholine esterase is 500 times higher than that to butyrylcholine esterase. The compound is shown to have an application prospect of being the medicines for curing Alzheimer's disease, cerebral vascular dementia, etc.