43 results about "Acetylcholine receptor" patented technology

The invention belongs to the technical field of synthetic chemistry, and provides a muscarinic acetylcholine receptor 3 fluorescent probe as well as a preparation method and application thereof. The chemical structural formula of the fluorescent probe is shown in the specification, and the fluorescent probe can be used for M3 receptor tracing in cells or organisms. The probe provided by the invention has a good fluorescent property and can be influenced by the polarity and viscosity of an external environment; and the probe has good biocompatibility, and the IC50 of the probe is 43 times of the concentration of a working solution, so that the probe can meet the requirements of cell fluorescence imaging. In the aspect of cell fluorescence imaging, the probe can realize selective fluorescence labeling of the M3 receptor in the cell, washing is not needed in the dyeing process, and the operation is simple and convenient, so that visual research on positioning of the M3 receptor in the cell is realized.

The invention provides therapeutic methods, pharmaceutical compositions, and unit dose formulations for treating movement disorders, such as using a muscarinic acetylcholine receptor inhibitor in combination with a muscarinic acetylcholine receptor activator to treat dystonia. In some aspects, the invention provides a method of treating a movement disorder in a patient, where the method comprises administering to a patient in need thereof (i) a muscarinic acetylcholine receptor inhibitor in an amount effective to treat the movement disorder and (ii) a muscarinic acetylcholine receptor activator in an amount effective to reduce the frequency and / or magnitude of at least one side effect of the muscarinic acetylcholine receptor inhibitor, to thereby treat the movement disorder.

This invention discloses a protein and gene related to resistance to neonicotinoid acetylcholine receptor competitive regulator insecticides in peach aphids, and their applications. It relates to the field of screening technology for neonicotinoid acetylcholine receptor competitive regulator insecticides in peach aphids. This invention obtains and clarifies an MpeABCC_4G protein and its encoding gene that is closely related to the resistance of peach aphids to neonicotinoid acetylcholine receptor competitive regulator insecticides. By knocking down the expression of MpeABCC_4G in resistant peach aphids using RNAi technology, the control efficacy of neonicotinoid acetylcholine receptor competitive regulator insecticides is significantly improved.

The invention relates to the field of medicinal chemistry, and discloses a sulfonyl derivative as well as a preparation method and application thereof. The compound provided by the invention and the composition containing the compound provided by the invention can be used for preparing medicines for diseases mediated by the mushroom type acetylcholine receptor.

To provide compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1), and methods for preparing the compounds.SOLUTION: The present invention provides a compound having the structure of formula (IA) or (IB), or a pharmaceutically acceptable salt or solvate thereof.SELECTED DRAWING: None

The invention relates to the technical field of medicinal chemistry, in particular to a 2-methyl-2-azabicyclo [3.2. 1] octane derivative which has a structure as shown in a general formula I or a general formula II or pharmaceutically acceptable salt, solvate, hydrate, isomer or prodrug of the 2-methyl-2-azabicyclo [3.2. 1] octane derivative, and a preparation method and application of the 2-methyl-2-azabicyclo [3.2. 1] octane derivative. As an acetylcholine receptor agonist, the compound shows high activity and high selectivity to M3 receptor subtypes. In-vitro experiments show that under the concentration of 40 mu M, the receptor excitation rate of the compound (such as 9a, 10a and the like) exceeds 95%, and is obviously superior to that of a positive control drug Aceclidine (48.65%). Due to the characteristic, the compound can generate a powerful pupil contraction pinhole effect by efficiently exciting an eye iris M3 receptor so as to improve near vision, and meanwhile, stimulation to ciliary muscles and related side effects are expected to be reduced due to high selectivity of the compound.

The present invention relates to novel pyrrolidinium compounds, stereoisomers, hydrates or solvates thereof, which exhibit excellent binding capacity and antagonistic activity to muscarinic receptors, in particular muscarinic M3 receptors. The compounds of the present invention are useful in the treatment of muscarinic acetylcholine receptor mediated diseases, such as hyperhidrosis, excessive salivation, chronic obstructive pulmonary disease, chronic bronchitis, asthma, rhinitis, urinary incontinence, overactive bladder, gastroesophageal reflux disease, irritable bowel syndrome, and the like.

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.

The present invention relates to a nucleic acid molecule for modulating neuromuscular transmission, said nucleic acid molecule comprising a sequence encoding one or more motor endplate receptors or fragments thereof. The present invention further relates to a fusion protein, preferably comprising one or more features of one or more of the foregoing Claims, said fusion protein comprising a motor endplate receptor and / or fragments thereof, wherein said motor endplate receptor is an acetylcholine receptor (AChR), a muscle-specific tyrosine kinase (MuSK) receptor, and / or a glutamate receptor, and / or fragments thereof, and / or a neurotoxin, wherein said neurotoxin is botulinum toxin (BoNT) and / or tetanus toxin.

The invention includes a chimeric autoantibody receptor (CAAR) specific for anti-acetylcholine receptor (AChR) B cell receptor (BCR), compositions comprising the CAAR, polynucleotides encoding the CAAR, vectors comprising a polynucleotide encoding the CAAR, and recombinant cells, e.g., T cells comprising the CAAR.

The present invention provides substituted tetrahydropyrrolo-pyridone compounds, pharmaceutical compositions and their use in the treatment of muscarinic acetylcholine receptor mediated conditions.

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 invention provides a muscarinic acetylcholine M4 receptor positive allosteric modulator as well as a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for preventing or treating muscarinic acetylcholine M4 receptor mediated related diseases, wherein the diseases comprise Alzheimer's disease, Parkinson's disease, schizophrenia, pain, addiction and sleep disorder.

The present invention provides substituted tetrahydropyrrolo-pyridinone compounds, pharmaceutical compositions, and their use in the treatment of muscarinic acetylcholine receptor-mediated disorders.

The invention relates to an anti-AchR (alpha) 1 subunit antibody and a preparation method thereof. The anti-AchR (alpha) 1 subunit antibody comprises a heavy chain variable region and a light chain variable region, the antibody is not only suitable for various experimental methods such as cellular immunofluorescence (IF) and tissue immunofluorescence (IHC), but also can specifically recognize the alpha 1 subunit of an AChR receptor, and especially shows efficient binding capacity to an AChR receptor protein complex. Due to the characteristics, the antibody can accurately reflect the real condition of combination of an in-vivo autoimmune antibody and an antigen, so that the antibody is very suitable for being used as a positive standard substance of an acetylcholine receptor autoantibody CBA detection kit.

The invention belongs to the field of biology and medicine, and relates to an alpha-conotoxin peptide LvID mutant as well as a pharmaceutical composition and application thereof. Specifically, the invention relates to a separated polypeptide which is a mutant of a polypeptide with an amino acid sequence as shown in SEQ ID NO: 1, and comprises the following mutations: E5A and Q11A. The separated polypeptide can specifically block the alpha7 acetylcholine receptor (nAChRs), has high selectivity and strong blocking activity on the alpha7 nAChRs, and has the potential of being used for preparing drugs for treating or preventing diseases related to the alpha7 nAChRs.

The invention provides therapeutic methods, pharmaceutical compositions, and unit dose formulations for treating movement disorders, such as using a muscarinic acetylcholine receptor inhibitor in combination with a muscarinic acetylcholine receptor activator to treat the movement disorder, such as dystonia. In some aspects, the invention provides a method of treating a movement disorder in a patient, where the method comprises administering to a patient in need thereof (i) a muscarinic acetylcholine receptor inhibitor in an amount effective to treat the movement disorder and (ii) a muscarinic acetylcholine receptor activator in an amount effective to reduce the frequency and / or magnitude of at least one side effect of the muscarinic acetylcholine receptor inhibitor, to thereby treat the movement disorder.

The present invention relates to novel pyrrolidinium compounds, stereoisomers thereof, hydrates thereof, or solvates thereof, which exhibit excellent binding ability and antagonistic activity to muscarinic receptors, particularly muscarinic M3 receptors. [Solution] The compounds of the present invention are useful in treating muscarinic acetylcholine receptor-mediated diseases such as hyperhidrosis, excessive salivation, chronic obstructive pulmonary disease, chronic bronchitis, asthma, rhinitis, urinary incontinence, overactive bladder syndrome, gastroesophageal reflux disease, and irritable bowel syndrome.

The application relates to the technical field of autoimmune disease in vitro diagnosis, and particularly relates to a recombinant expression vector for inducing expression of clustered acetylcholine receptors, a double-stable cell strain and application thereof. The recombinant expression vector is a tetracycline-inducible expression vector for single-carrier multi-subunit independent expression; the vector is integrated with acetylcholine receptor full-subunit coding sequence and Rapsyn protein coding sequence through an iterative enzyme cutting-linking mode, wherein each to-be-inserted subunit independent expression box is respectively provided with I-CeuI enzyme cutting sites and BstXI enzyme cutting sites at two ends, and each subunit and Rapsyn protein are driven to express by an independent Tet-On inducible promoter after iterative linking. Through the core design of single-carrier multi-subunit independent expression and Tet-On tetracycline induction regulation, the acetylcholine receptor pentamer assembly efficiency, the stable cell strain passage stability and the anti-AChR antibody detection performance are greatly improved.

This invention belongs to the field of biomedicine and relates to a novel α-conotoxin peptide LvIE and LvIF, its pharmaceutical composition, and its uses. An isolated polypeptide has an amino acid sequence as shown in any one of SEQ ID NOs:4-5 and SEQ ID NOs:7-8. The α-conotoxin peptide of this invention can effectively and specifically block α3β2 acetylcholine receptors and α6β2*nAChRs acetylcholine receptors, and has the potential to prevent and treat neuralgia, addiction, Parkinson's disease, dementia, schizophrenia, or depression, showing promising application prospects.

The invention relates to a fluorescent probe based on a quantum dot fluorescence resonance energy transfer effect, a preparation method of the fluorescent probe and a method for detecting an acetylcholine receptor antibody by using the probe. The method comprises the following steps: preparing particle size monodisperse carrier microspheres through a template method, then carrying out surface modification on the carrier microspheres and quantum dots, so that the quantum dots are attached to the surfaces of the carrier microspheres through electrostatic self-assembly or hydrophobic driving assembly to form quantum dot microspheres; the preparation method comprises the following steps: preparing a quantum dot microsphere, performing carboxyl modification on the surface of the quantum dot microsphere, activating, coupling an acetylcholine receptor antigen to the surface of the quantum dot microsphere, and sealing a non-specific binding site by using a sealing agent to obtain a quantum dot microsphere labeled AchR antigen as a fluorescent probe. The immobilization of the cross-linking agent enhances the binding strength between the quantum dots and the carrier microspheres, and closes non-specific binding sites on the surfaces of the microspheres, thereby ensuring the structural stability of the probe. In addition, an AchR-Ab detection method using the quantum dot FRET fluorescent probe provided by the invention can realize quantitative detection of AchR-Ab concentration.

The invention discloses a synergistic composition containing isoxazoline insecticidal and acaricide, which is composed of a compound I and a compound II, the compound I is CCXN-15-005-S (S configuration) or an agrochemically acceptable salt thereof, and the compound II is CCXN-15-005-S (S configuration) or an agrochemically acceptable salt thereof. The compound II is selected from any one of a nicotinic acetylcholine receptor agonist, a chordinal TRPV channel regulator, an acetyl-coenzyme A carboxylase (ACCase) inhibitor, a mitochondrial electron transfer inhibitor, a calcium-activated potassium ion channel regulator and trifluoroethyl thioether (sulfoxide) or an agrochemically acceptable salt thereof. The synergistic composition can be used for preventing and treating pests and harmful mites of thysanoptera, hemiptera and acarus and has a wider agricultural application prospect.

The invention belongs to the technical field of biological medicines, and relates to a spiro polypeptide with a single disulfide bond and a mutant and application thereof. The amino acid sequence of the conotoxin polypeptide is shown as SEQ ID NO.1 in a sequence table. One or more amino acid site-directed mutagenesis is carried out on the amino acid sequence of the conotoxin polypeptide to obtain a series of mutants. A plurality of mutants have better inhibitory activity and selectivity on an alpha9alpha10 acetylcholine receptor; wherein the IC50 of the M16R is 28.2 nM, and the IC50 of the F19R is 17.5 nM. In addition, M16R and F19R show in-vivo analgesic activity in a chemotherapeutic drug oxaliplatin induced rat crymodynia model, and have the potential of being developed into a neuropathic pain treatment drug targeting alpha9alpha10nAChR.

Ophthalmically-acceptable formulations of atropine and other muscarinic acetylcholine receptor antagonists are provided that can be heat-sterilized without significant degradation of the muscarinic acetylcholine receptor antagonist. The formulations are less acidic than prior muscarinic acetylcholine receptor antagonist ophthalmic formulations, making them more comfortable when administered to the eye.

The invention provides a muscarinic acetylcholine M4 receptor positive allosteric modulator as well as a preparation method and a pharmaceutical composition thereof. The invention also relates to application of the compound or the pharmaceutical composition in preparation of drugs for preventing or treating muscarinic acetylcholine M4 receptor mediated related diseases, wherein the diseases comprise Alzheimer's disease, Parkinson's disease, schizophrenia, pain, addiction and sleep disorder.

The invention discloses a tetrahydrofuran compound, or an enantiomer, a raceme or a mixture form of the tetrahydrofuran compound, or pharmaceutically acceptable salt, a deuterated substance, a solvate, a hydrate and a metabolite of the tetrahydrofuran compound, and a pharmaceutical composition and application of the tetrahydrofuran compound. The tetrahydrofuran compound provided by the invention has good excitation activity on a Sigma-1 receptor and an M-type acetylcholine receptor, and has a good treatment effect on central nervous system diseases.

The invention provides therapeutic methods, pharmaceutical compositions, and unit dose formulations for treating movement disorders, such as using a muscarinic acetylcholine receptor inhibitor in combination with a muscarinic acetylcholine receptor activator to treat dystonia. In some aspects, the invention provides a method of treating a movement disorder in a patient, where the method comprises administering to a patient in need thereof (i) a muscarinic acetylcholine receptor inhibitor in an amount effective to treat the movement disorder and (ii) a muscarinic acetylcholine receptor activator in an amount effective to reduce the frequency and / or magnitude of at least one side effect of the muscarinic acetylcholine receptor inhibitor, to thereby treat the movement disorder.

The invention discloses an application of an acetylcholine receptor stimulant in treatment of meningitis. It is found for the first time that the acetylcholine receptor stimulant GTS-21 can prevent and treat meningitis and can also prevent and treat cognitive impairment caused by meningitis, a new thought is provided for effective treatment of meningitis and memory impairment caused by meningitis, and the acetylcholine receptor stimulant GTS-21 has wide application prospects.

An ophthalmically-acceptable aqueous liquid composition is provided comprising an amine buffer and a muscarinic acetylcholine receptor antagonist which comprises a hydrolysable bond wherein the muscar

The present invention provides substituted dihydropyrrolo-pyrimidine compounds, pharmaceutical compositions and their use in the treatment of muscarinic acetylcholine receptor mediated conditions, including cancer.