53 results about "Acetylcholine" patented technology

The present application relates to a kind of thieno [2, 3-c] pyridazine derivatives, and its isotope form, stereoisomer, tautomer, cis-trans isomer, pharmaceutically acceptable salt, pharmaceutically acceptable solvate, hydrate, prodrug and polymorph, these compounds can be used as cholinergic M4 receptor positive allosteric modulator, it has good application prospect in preparation for preventing and / or treating the drug for the disease related to abnormal muscarinic acetylcholine receptor.

The application discloses a kind of photoactivation manganese ion bridging type deoxyribozyme probe preparation and its application in Cistanche inhibiting acetylcholinesterase activity.The probe is pSD@MnO2 Composite structure, which is composed of manganese dioxide nanosheet and functional nucleic acid assembly adsorbed on its surface, the assembly includes S chain labeled with fluorescence / quenching group and containing deoxyribozyme cleavage site, and pD chain partially hybridized with S chain and containing photocleavage site.Its preparation includes nucleic acid probe assembly, MnO2 Nanosheet complexing and purification steps.When applied, AChE catalytic product decomposes MnO2, releases Mn 2+ And nucleic acid chain; after centrifugation, pD chain is cut by ultraviolet light activation trigger, and released DNAzyme is cut under the assistance of Mn 2+ It produces amplified fluorescence signal; by comparing signal change before and after adding inhibitor, inhibition activity can be quantitatively evaluated.The application combines photocontrol activation with enzyme cascade amplification, realizes high sensitivity and operation synchronism of detection process, and is especially suitable for high-throughput rapid screening of AChE inhibitor in Cistanche and other natural products.

The application provides a neural snake venom poisoning discrimination data processing method and system based on neural electrical signals, and relates to the technical field of signal processing. The method comprises the following steps: converting the neural electrical signals of a subject into a digitized multi-channel time sequence matrix; obtaining a multi-channel time sequence signal through band-pass filtering, power interference suppression, hierarchical artifact removal, baseline correction and resampling; extracting time domain, frequency domain, time-frequency domain and synapse and neuromuscular transmission characteristics, wherein the characteristics include four train-of-four ratios, repetitive nerve stimulation response decrement rates, acetylcholine release frequencies and amplitude variation coefficients corresponding to acetylcholine release; standardizing the characteristics and performing dimensionality reduction by principal component analysis to obtain an optimized characteristic set; inputting a pre-trained poisoning discrimination model to output poisoning probability, confidence and key abnormal characteristics. The application solves the problem that the prior art lacks a specific processing flow and a full-process engineering scheme for neural snake venom poisoning, resulting in low discrimination accuracy and difficulty in meeting emergency clinical needs.

The present invention provides an ocular drug delivery method comprising the method step of topically administering to the skin of the eyelids of a subject a therapeutically effective amount of a pharmaceutical composition, wherein the pharmaceutical composition comprises: (a) a therapeutically active agent comprising a muscarinic acetylcholine receptor (mAChRs) modulator; and (b) a pharmaceutically acceptable carrier.

This invention discloses a biosensor membrane for the detection of organophosphorus pesticides, comprising a base membrane on which multiple glucose oxidase catalytic modules and multiple acetylcholinesterase catalytic modules are loaded. Each glucose oxidase catalytic module includes a first carrier immobilized on the base membrane and glucose oxidase loaded thereon. Each acetylcholinesterase catalytic module includes a second carrier immobilized on the base membrane and acetylcholinesterase loaded thereon. The weight ratio of glucose oxidase to acetylcholinesterase is 1:1 to 1:4. This invention reveals the structure-activity relationship of enzyme ratio-enzyme load synergistic regulation of sensing interface performance. By establishing a competitive inhibition advantage through changing the enzyme ratio, the enzyme load is optimized to achieve a balance between high activity and high mass transfer, thereby synergistically improving signal change and inhibition rate, achieving highly sensitive detection of organophosphorus pesticides. The biosensor membrane provided by this invention is suitable for the detection of various organophosphorus pesticides in food (especially crops and dairy products).

The invention provides a method of diagnosing overactive bladder disorder (OAB), the method comprising: measuring the concentrations of one or more of adenosine triphosphate (ATP), acetylcholine (ACh), nitric oxide (NO) and interleukin 5 (IL-5) in a sample obtained from a subject; normalising the concentrations to the concentration of creatinine (Cr) in the sample; range standardising the normalised concentrations and subject's age to the following values: Age to 120 years old; ATP / Cr to 0.000001; ACh / Cr to 0.1; NO to 20000; IL-5 / Cr to 100; wherein the likelihood of having OAB (pOAB)=1 / 1+e−x, where X=one or more of the following: (a) (−2.688±1.050)+5.472±2.098×subject's age+1.356±0.559×Gender (Female=1, Male=0)+(−7.998±40.273)×[IL-5 / Cr]; (b) (−2.141±0.966)+4.506±1.902×subject's age+1.034±0.519×Gender (Female=1, Male=0)+(−5294.063±9075.456)×[ACh / Cr]; (c) (−2.825±1.072)+5.964±2.167×subject's age+1.312±0.562×Gender (Female=1, Male=0)+17.790±58.762×[IL-5 / Cr]+(−9180.821±12700.057)×[ACh / Cr]; (d) (−2.993±1.197)+5.580±2.309×subject's age+1.724±0.719×Gender (Female=1, Male=0)+63.571±73.444×[IL-5 / Cr]+(−0908.523±13606.752)×[ACh / Cr]+(−566.991±636.589)×[ATP / Cr]; (e) (−3.090±1.200)+5.393±2.256×subject's age+1.797±0.717×Gender (Female=1, Male=0)+34.767±56.331×[IL-5 / Cr]+(−562.743±629.316)×[ATP / Cr]; or (f) (−2.650±1.067)+5.516±2.120×subject's age+1.389±0.583×Gender (Female=1, Male=0)+(−4.060±45.238)×[IL-5 / Cr]+(−1.456±6.833)×[NO / Cr]; and wherein a pOAB above a threshold indicates that the subject has a high likelihood of having or developing OAB and a pOAB below a threshold indicates that the subject does not have OAB.

The present invention relates to compounds of formula (Ia), pharmaceutically acceptable salts of compounds of formula (Ia), and pharmaceutical compositions thereof that modulate the activity of the muscarinic acetylcholine receptor M4. The compounds, pharmaceutical salts of compounds, and pharmaceutical compositions of the present invention are directed to methods useful in the treatment or prophylaxis of a neurological disease, disorder, or symptom, and conditions related thereto.

Provided herein, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

This invention belongs to the field of pharmaceutical technology and relates to eight glycoside compounds extracted and isolated from the dried leaves of *Picrasma quassioides* Benn, a plant belonging to the genus *Picrasma* in the family Simaroubaceae. The compounds were obtained using chromatographic methods including silica gel chromatography, HP20 column chromatography, ODS column chromatography, and HPLC. This invention also relates to the acetylcholinesterase inhibitory activity of compounds 1-8 and their pharmaceutical uses. The preparation method of this invention is simple, reproducible, and of high purity.

The present invention relates to the field of probiotics, in particular to an Akkermansia muciniphila MG784 for alleviating constipation, promoting defecation, improving intestinal barrier function and intestinal immunity, and its uses. The Akkermansia muciniphila MG784 provided by the present invention has the deposition number DSM 35549. The Akkermansia muciniphila MG784 provided by the present invention can increase the levels of motilin (MTL), gastrin (GAS), and acetylcholine in the gastrointestinal tract, promote intestinal peristalsis, improve the small intestine propulsion rate, and ameliorate defecation time and fecal output. Furthermore, Akkermansia muciniphila MG784 can also alleviate colonic mucosal inflammation, improve the thickness of the digestive tract muscular layer, modulate the structure of the intestinal microbiota, significantly increase the abundance of beneficial bacteria, and decrease the abundance of harmful bacteria.

The present invention relates to a cyclic derivative, a preparation method therefor and the use thereof. The cyclic derivative can be used as a muscarinic acetylcholine receptor agonist and / or a Sigma receptor agonist, or can be used for treating schizophrenia, Parkinson's disease, Alzheimer's disease, depression and other neuropsychiatric diseases.

This invention belongs to the field of biotechnology, specifically relating to the acetylcholine receptor of the root-knot nematode *Eupolyphaga sinensis*. unc38 Genes, their dsRNAs, and applications. To provide novel target genes for the control of *Eriocheir sinensis* root-knot nematode, this invention is based on the *Eriocheir sinensis* acetylcholine receptor... unc38 Gene SEQ ID NO:1 was used to design and synthesize gene fragment SEQ ID NO:5 and the corresponding dsRNA. The synthesized dsRNA was used to soak second-instar root-knot nematodes. unc38 Gene expression levels were downregulated, resulting in a mortality rate of 68.9% at 60 hours, and complete death of nematodes at 120 hours. Immersion unc38 The dsRNA-infected second-instar larvae of the bean root-knot nematode significantly reduced the infectivity of tomato roots. After 30 days of inoculation, the number of root knots decreased significantly by about 57%, and the number of females, the number of egg masses, the number of eggs in each egg mass, and reproductive factors were all significantly reduced.

The application belongs to the technical field of biosensing and specifically relates to a biosensor for detecting active acetylcholinesterase and application thereof. The biosensor comprises nanotubes with nanometer apertures at tips for generating current blocking signals; and a ring bundle DNA tetrahedron carrier for loading a solution containing active acetylcholinesterase to be detected, wherein the ring bundle DNA tetrahedron carrier is TDN1 or TDN4, the sequences of the four DNA single strands in TDN1 are shown as SEQ ID NO. 1 to SEQ ID NO. 4, and the sequences of the four DNA single strands in TDN4 are shown as SEQ ID NO. 1, SEQ ID NO. 3, SEQ ID NO. 5 and SEQ ID NO. 6. The application utilizes a closed-loop DNA tetrahedron nanostructure anchored at two ends of an aptamer to generate a difference in current signals in a nanometer hole before and after the active AChE is combined, so that high-sensitivity and high-selectivity detection of the active AChE at a single-molecule level is achieved.

The invention relates to compositions and methods for producing and using antibodies against the alpha7 nicotinic acetylcholine receptor.

This invention discloses alkaloid compounds from Brucea javanica, their preparation methods, and applications, belonging to the field of pharmaceutical technology. Specifically, it relates to two alkaloid compounds extracted and isolated from the fruit of Brucea javanica, a plant of the genus Brucea in the family Simaroubaceae. These compounds have good acetylcholinesterase inhibitory activity and can be used to prepare acetylcholinesterase inhibitors, showing good development prospects and application potential.

N-Biarylmethylene substituted pyrrolopyridinone, pyrrolopyrazinone, pyrrolopyrimidinone, and isoindolin-1-one compounds having a tertiary alcohol-containing group substituted on the biarylmethylene are positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChRM1). The compounds and pharmaceutical compositions may be used in treating neurological disorders, psychiatric disorders, or a combination thereof.

The application discloses a benzofuran glycoside compound, a separation and extraction method thereof, a pharmaceutical composition and application, and the compound 1 is separated from a macleaya cordata extract. A benzofuran compound is obtained by separating and purifying a n-butanol part chemical component of a macleaya cordata root. The inhibitory activity of all separated compounds 1 on a target point cyclooxygenase-2 of an inflammatory related disease is tested, the compound 1 has good inhibitory activity on COX-2 enzyme, and the compound 1 has better binding energy with the target point protein. The compound also has good NLRP3 related inhibitory effect, can be used alone or in combination with other drugs to regulate NLRP3 related proteins, is used for treating NLRP3 related mediated diseases and / or diseases, and is used for preparing drugs for preventing or treating the diseases. The compound 1 also has better inhibitory effect on acetylcholinesterase, and can be used for treating diseases such as Alzheimer's disease, myasthenia gravis and Parkinson's disease.

This invention belongs to the field of pesticide technology, specifically relating to an insecticidal composition containing cybenzoxasulfyl and its application. The insecticidal composition comprises active ingredient A and active ingredient B, wherein active ingredient A is cybenzoxasulfyl; active ingredient B is selected from one or more of the following compounds: acetylcholinesterase inhibitors, nicotinic acetylcholine receptor (nAChR) channel blockers, nicotinic acetylcholine receptor (nAChR) allosteric modulator site I, nicotinic acetylcholine receptor (nAChR) competitive modulators, glutamate-gated chloride channel (GluCl) allosteric modulators, etc. This composition has a reasonable composition, good insecticidal effect, low application cost, and features reduced application amount, crop safety, and reduced pesticide residues.

This invention discloses the use of cyanidin anthocyanins or their pharmaceutically acceptable salts, esters, and solvates in the preparation of drugs for the prevention and / or treatment of neurodegenerative diseases. The cyanidin anthocyanins are selected from cyanidin-3-O-rutin glycoside, cyanidin-3-O-sophoroside, or cyanidin-3-O-xyloside. These compounds can inhibit acetylcholinesterase activity, upregulate α7 nicotinic acetylcholine receptor expression, and activate the PI3K / AKT / GSK3β signaling pathway, thereby inhibiting Tau protein hyperphosphorylation and reducing neuroinflammatory responses. Furthermore, it has been confirmed that cyanidin-3-O-rutin glycoside directly binds to acetylcholinesterase, verifying AChE as its key target, providing new natural active compounds and their mechanisms of action for the prevention and treatment of neurodegenerative diseases.

This invention relates to a ventilation detection device for patients with myasthenia gravis based on testing and detection, comprising: a muscle strength monitoring module, including an electromyography (EMG) sensor for acquiring EMG signals and calculating a muscle strength index; a respiratory monitoring module, connected to a mechanical ventilation device, for acquiring the patient's respiratory rate, tidal volume, and inspiratory time parameters; a blood detection module for collecting blood samples from the patient and detecting the levels of inflammatory factors and anti-acetylcholine receptor antibodies in the blood; and a control module for receiving muscle strength index data, respiratory parameter change trend data, and blood detection data; when the muscle strength index is lower than a preset first threshold, the respiratory parameter change trend is inconsistent with a preset pattern, and the levels of inflammatory factors or anti-acetylcholine receptor antibodies in the blood are higher than a preset second threshold, patient-ventilator resistance is determined to exist during ventilation.

This invention provides a material for detecting serum plasma anti-nicotinic acetylcholine receptor antibodies and its method of use. The material comprises HEK293T cells transfected with three recombinant expression plasmids: the first plasmid encodes a truncated AChR α subunit; the second plasmid is a polycistronic plasmid encoding a fusion protein composed of a truncated AChR β subunit, an AChR δ subunit, and rapsyn protein linked by a P2A peptide; and the third plasmid encodes a truncated AChR γ subunit or ε subunit. After co-transfection with PEI, the cells are cultured in fresh complete medium for 25-35 hours after 7-9 hours post-transfection, followed by fixation, blocking, and preservation. This invention, through a three-plasmid system and antigen truncation modification, reduces cytotoxicity while ensuring high expression of the functional pentamer, significantly improving detection sensitivity and reagent shelf life.

An insecticidal composition containing cybenzoxasulfyl and the use thereof. The insecticidal composition contains active ingredient A and active ingredient B, wherein active ingredient A is cybenzoxasulfyl, and active ingredient B is selected from one or more of the following compounds: an acetylcholinesterase inhibitor, a nicotinic acetylcholine receptor (nAChR) channel blocker, nicotinic acetylcholine receptor (nAChR) allosteric modulator site I, a nicotinic acetylcholine receptor (nAChR) competitive modulator, a glutamate-gated chloride channel (GluCl) allosteric modulator, etc. The composition has reasonable components, good insecticidal effects, and low administration costs, and also has the characteristics of a reduced application amount, safety to crops, reduced pesticide residues, etc.

Methods of accelerating clot formation and increasing clot deposition in a hemophiliac subject. A vagal nerve stimulator (VNS) may be implanted in a hemophiliac subject. The hemophiliac subject may have developed antibodies to factor VIII and not been administered a clotting factor within the last 48 hours. The vagus nerve of the subject may be stimulated in a manner that increases platelet intracellular calcium and / or activates splenic acetylcholine-synthesizing T lymphocytes using the implanted VNS.

The present application relates to the field of microorganisms, and provides a propionibacterium acidifaciens BL8 with functions of reducing blood sugar and resisting aging, and application thereof, the propionibacterium acidifaciens BL8 is preserved in China General Microbiological Culture Collection Center on December 20, 2024, and the preservation number is CGMCC No.33134.The propionibacterium acidifaciens BL8 of the present application can inhibit DPP4 activity, promote INS-1 insulin secretion, inhibit acetylcholinesterase activity and superior cellulase activity.Can reduce blood sugar;Improve memory, prevent and relieve Alzheimer's disease;Promote cellulose absorption, improve constipation, and have high research and application value in reducing blood sugar and resisting aging.

The application discloses a kind of chess nan linaloe leaf flavonoids compound extraction purification method and application.It belongs to flavonoids extraction technical field.The application extracts flavonoids compound in chess nan linaloe leaf by ultrasonic wave auxiliary ethanol extraction method, and is determined by single factor test and response surface method optimization optimum extraction process;Further, macroporous adsorption resin is used to purify crude extract, and obtain purified flavonoids compound.Flavonoids compound contains many active ingredients such as acacia leaf glycoside, quercetin, sakura flower element by identification.The method of the application is high in extraction efficiency, simple in operation, environmentally friendly and safe, and the obtained flavonoids compound has significant antioxidant activity and inhibitory activity of acetylcholinesterase and alpha-glucosidase, which provides technical support for the development and utilization of chess nan linaloe leaf.

The present invention provides lateral flow assay devices and methods for detecting nicotinic acetylcholine receptor ligands in liquid samples. The device comprises a porous strip with multiple zones, including a sample deposition zone, a test visualization zone containing an immobilized nicotine conjugate, a control zone, and an absorbent zone. A recombinant acetylcholine receptor protein serves as a mobile agent, either pre-deposited on the strip or added to the sample. The recombinant protein comprises a ligand-binding domain of a nicotinic acetylcholine receptor conjugated to a visually-detectable reporter forming a receptor-reporter conjugate. When nicotinic acetylcholine receptor ligands are present in the sample, they competitively bind to the recombinant receptor protein, reducing binding to the immobilized nicotine conjugate and producing a visually detectable signal inversely proportional to ligand concentration. The invention provides rapid, simple, and field-deployable detection of receptor ligands in environmental samples, including cyanobacterial neurotoxins in surface waters, and biological samples for pharmacological and toxicological applications.