27 results about "Acetylcholine receptor" patented technology

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.

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 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.

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 invention provides substituted tetrahydropyrrolo-pyridinone compounds, pharmaceutical compositions, and their use in treating muscarinic acetylcholine receptor mediated disorders.

The invention relates to muscarinic acetylcholine M1 receptor antagonists. Provided herein, inter alia, are compounds useful as antagonists of muscarinic acetylcholine receptor M1 (mAChRM1); synthetic methods for preparing the compounds; a pharmaceutical composition including the compound; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and the compositions.

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

The invention relates to compositions and methods for chimeric autoantibody recipient cells of acetylcholine receptors. The present invention includes chimeric autoantibody receptors (CAARs) having specificity against acetylcholine receptor (AChR) B cell receptor (BCR), compositions comprising the CAARs, polynucleotides encoding the CAARs, vectors and recombinant cells comprising the polynucleotides encoding the CAARs, e.g., T cells comprising the CAARs.

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.