31 results about "Antagonism" patented technology

Provided are a compound having serotonin 5-HT2A receptor antagonism and / or inverse agonism, a pharmaceutically acceptable salt thereof, and a composition for serotonin 5-HT2A receptor antagonism and / or inverse agonism comprising them.A compound represented by Formula (I):wherein R1 is substituted or unsubstituted aromatic heterocyclyl or the like; R2 is each independently a hydrogen atom or the like; R3 is each independently a hydrogen atom or the like; n is 1 or the like; a combination of (L1, L2) is (NH, N) or the like; R4 is a group represented by Formula:wherein p and q are each independently 2 or the like; Ra is substituted or unsubstituted alkyl or the like; Xb is each independently CRbRb′; Rb is each independently a hydrogen atom or the like; Rb′ is each independently a hydrogen atom or the like; Xc is each independently CRcRc′; Rc is each independently a hydrogen atom or the like; Rc′ is each independently a hydrogen atom or the like; Xd is CRd or the like; and Rd is a hydrogen atom or the like; R5 and R6 are each independently a hydrogen atom or the like; and R7 is a group represented by Formula:wherein A is CR11 or the like; R9 is substituted or unsubstituted alkyloxy or the like; R10 is a hydrogen atom or the like; and R11 is each independently a hydrogen atom or the like; or a pharmaceutically acceptable salt thereof.

This invention provides a pharmaceutical product for the prevention and / or treatment of pain, particularly neuropathic pain associated with multiple sclerosis, containing compounds with P2X4 receptor antagonism, such as compounds represented by general formula (IH), or their salts, or their hydrates or solvates, as active ingredients.

This invention discloses a vascular bundle-targeted bio-selenium nanoparticle, its preparation method, and its application, belonging to the field of plant treatment technology. The invention involves mixing and dissolving bio-selenium nanoparticles, water, 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride, and N-hydroxysuccinimide, followed by activation to obtain an activated bio-selenium nanoparticle solution. A xylem-anchored peptide and MES buffer are then mixed and dissolved to obtain a xylem-anchored peptide solution. The activated bio-selenium nanoparticle solution and the xylem-anchored peptide solution are mixed, and the pH is adjusted to 6.3-6.8 before stirring to obtain the vascular bundle-targeted bio-selenium nanoparticle. The vascular bundle-targeted bio-selenium nanoparticle provided by this invention achieves interception of heavy metal transport pathways by specifically anchoring to xylem vessels. Compared with existing technologies that rely solely on broad-spectrum physiological antagonism, its efficiency in reducing heavy metal content in crop stems and leaves represents a qualitative leap.

The present application belongs to the technical field of polypeptide drugs, and particularly relates to a kind of small molecule polypeptide and its application in psoriasis treatment.The present application successfully designs and synthesizes a kind of small molecule polypeptide OGP6 with the effect of intervening psoriasis.By test verification, it can effectively target inhibition cGAS-STING signal pathway, intervene psoriasis inflammation start from source, avoid the existing biological preparation long-term antagonism single cytokine to cause the problem such as drug resistance antibody production, curative effect invalidation, and its still has the advantages such as small molecular weight, simple synthesis process, low cost, easy to scale production, therefore has good practical application value.

An object of the present invention to provide a clozapine-induced sialorrhea alleviator. The clozapine-induced sialorrhea alleviator of the present invention contains as an active ingredient dextromethorphan, a compound having an antagonistic action on an NMDA-type glutamate receptor, or a compound having an agonistic action on a sigma-1 receptor.

The application discloses a plant extraction compound for reducing blood pressure, a preparation method and application thereof. The compound is composed of high-purity silybin extract and a specific fusion polypeptide through molecular self-assembly. The sequence of the fusion polypeptide is shown in sequence SEQ ID NO:1, which innovatively integrates cell membrane penetration function, angiotensin II receptor 1 antagonism function and hydrophobic drug binding function. The core of the application is that through polypeptide-mediated active targeting, silybin is accurately delivered to the diseased blood vessel area, and the double synergistic mechanism of upstream ACE inhibition and downstream receptor blocking of the renin-angiotensin-aldosterone system is realized. In-vivo pharmacodynamic experiments prove that compared with single components, the compound can produce more significant and persistent antihypertensive effect, and can effectively reverse myocardial hypertrophy and fibrosis caused by hypertension, and show excellent synergistic therapeutic effect and target organ protection ability.

The present invention relates to a dual-targeting siRNA agent comprising two distinct siRNAs targeting two different genes or their pharmaceutically acceptable salts, wherein the two distinct siRNAs or their salts are linked by a pharmaceutically acceptable ligand. The siRNA is a dsRNA composed of a sense strand and an antisense strand, and the two different genes are selected from a group consisting of angiotensinogen (AGT), proprotein convertase subtilisin / kexin type 9 (PCSK9), and human angiopoietin-like protein 3 (ANGPTL3). The present invention provides the application of the dual-targeting siRNA agent in the preparation of drugs for preventing or treating diseases associated with hypertension and / or dyslipidemia. The dual-targeting siRNA agent described in the present invention can effectively inhibit the expression of two target genes simultaneously in vivo, offering the advantages of strong non-antagonistic activity and high safety. The present invention also provides the siRNAs targeting corresponding genes for the aforementioned dual-targeting siRNA agent and their use for preventing or treating diseases associated with hypertension and / or dyslipidemia.

Provided in the present invention are a compound as shown in formula IA, a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug thereof. The compound has a good MRGPRX2 antagonistic effect.

The present invention provides histamine H1 receptor antagonism-based uses for various uses (histamine H1 receptor antagonism uses, uses to improve sleep quality and / or modulate balance of the autonomic nervous system, and uses to improve sleep quality and / or modulate balance of the autonomic nervous system. And a use for preventing the onset of autonomic nervous system dysfunction or a symptom caused thereby or for improving autonomic nervous system dysfunction or a symptom caused thereby). The present invention relates to: a composition comprising, as an active ingredient, at least one substance selected from the group consisting of indole-3-lactic acid, alpha-Asp-Phe, Val-Arg, Asp-Gly-Glu, and salts thereof, or a lactic acid bacteria culture supernatant (not containing lactic acid bacteria cells) of a lactic acid bacteria belonging to any genus selected from the group consisting of the genus Lactobacillus, the genus Lactobacillus, and the genus Lactobacillus; the liquid supernatant contains at least one substance selected from the group consisting of indole-3-lactic acid, alpha-Asp-Phe, Val-Arg, Asp-Gly-Glu, and salts thereof. The liquid supernatant contains at least one substance selected from the group consisting of indole-3-lactic acid, alpha-Asp-Phe, Val-Arg, Asp-Gly-Glu.

This invention discloses polypeptides or their salts, their preparation methods, and applications, belonging to the field of biotechnology. The polypeptide or its salt according to formula (I) has the following structure: L-methionyl-L-prolyl-D-phenylalanyl-L-arginyl-D-tryptophanyl-L-phenylalanyl-X-L-prolyl-L-valine (I); wherein X is a 4-(aminomethyl)cyclohexane carbonyl group. The polypeptide or its salt of this invention exhibits both antagonistic activity against MC1R receptors and inhibitory activity against tyrosinase, with perfect temporal and spatial synergy, thereby effectively inhibiting melanin production in the skin and improving hyperpigmentation.

The present application relates to the technical field of inhalation anesthetic antagonism, and particularly relates to the application of a corticotropin-releasing hormone receptor antagonist in the preparation of an inhalation anesthetic antagonist. The present application first discovers that the corticotropin-releasing hormone receptor of the dorsal raphe nucleus is a key target of the action of an inhalation anesthetic, and that the oculomotor nerve parvocellular nucleus-dorsal raphe nucleus neural loop mediates the effect of an inhalation anesthetic, and that a corticotropin-releasing hormone receptor antagonist can block the excitatory effect of urocortin on the neurons of the dorsal raphe nucleus, thereby weakening the effect of an inhalation anesthetic. The present application first applies a corticotropin-releasing hormone receptor antagonist in the preparation of an inhalation anesthetic antagonist, fills the technical gap in this field, is conducive to the rapid postoperative recovery of patients under general anesthesia, and has a broad application prospect.

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and / or hydrate and / or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon-like peptide-1 receptor (“GLP-1R”) and / or the gastric inhibitory polypeptide receptor (“GIPR”). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP-1R and / or GIPR activities is beneficial for the treatment or prevention of the underlying pathology and / or symptoms and / or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancement of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP-1R and / or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple) β-arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.

This invention, entitled "Combined Application and Product of BAM-15 and Erlotinib," belongs to the field of combined antitumor drug application technology. The technical problem it aims to solve is the low response and limited efficacy of existing erlotinib monotherapy to EGFR wild-type lung adenocarcinoma, and the lack of effective targeted intervention options in clinical practice. The key points of the technical solution are: combining BAM-15 and erlotinib for the interventional treatment of EGFR wild-type lung adenocarcinoma; the combination produces a significant synergistic effect, with tumor suppression superior to the additive effect of using either drug alone, without antagonistic effects, effectively enhancing the inhibitory effect on EGFR wild-type lung adenocarcinoma and enriching clinical treatment options for tumors.

The present application relates to the technical field of medicine, and particularly relates to application of OpiCa1 or a nano-liposome thereof in preparation of a drug for treating and / or preventing myocardial fibrosis related diseases. The present application is found that OpiCa1 and the nano-liposome thereof can inhibit myocardial fibrosis and improve myocardial remodeling in the myocardial remodeling period after myocardial infarction, and have a good antagonistic effect on myocardial infarction and subsequent heart failure. Further transcriptomic analysis shows that in the process of treating myocardial infarction in mice, OpiCa1 and the nano-liposome thereof can inhibit fibrosis and improve myocardial remodeling by possibly participating in extracellular matrix degradation in myocardial remodeling and fibrosis pathways (such as TGF-beta signaling pathway), so as to achieve the purpose of relieving myocardial infarction deterioration.

The present application relates to a kind of can prevent and treat bacterial wilt of lemon acid-loving Leuconostoc Q2-1, on February 9, 2026, be preserved in China Microorganism Strain Preservation Management Committee, and the application also relates to the application of the lemon acid-loving Leuconostoc Q2-1 in the prevention and treatment of bacterial wilt.The antagonistic strain Q2-1 of the present application is isolated from the rhizosphere of plant, and it is a kind of harmless strain to human and animal and plant, and the strain has significant antagonism to ralstonia solanacearum.In addition, volatile metabolites of antagonistic strain Q2-1 are analyzed by its plate bacteriostatic analysis, and it is found that certain metabolites in the gas produced by antagonistic strain Q2-1 have inhibitory effect on bacterial wilt pathogen CQPS-1.Therefore, the antagonistic strain Q2-1 of the present application has prevention and treatment effect on bacterial wilt of solanaceae crops, provides a new effective way for the prevention and treatment of bacterial wilt of solanaceae crops, and has good application prospect.

The present invention provides a TSHR antagonist compound of formula (I), a pharmaceutical composition, a method for preparing same, and use thereof. The compound has a good TSHR antagonistic effect and is used for treating thyroid-related disorders and / or diseases, such as hyperthyroidism, Graves' disease, Graves' ophthalmopathy, and thyroid-associated ophthalmopathy, and for preparing a medicament for such disorders or diseases.

The application belongs to the technical field of biological medicine, and particularly relates to a compound for treating androgenic acne and alopecia and preparation and application thereof. The compound is a 17alpha, 21-diester compound of 11-deoxycortisol and a pharmaceutically acceptable salt thereof, and a structural general formula of the compound is as follows: wherein R is selected from C(O)-R1; R1 is an alkyl acid containing 3 or 8 carbon atoms. The compound has good stability, has different degrees of antagonism on androgen receptors, can be used for preparing a medicine for treating acne and androgenic alopecia, and has a good application prospect.

This invention belongs to the interdisciplinary field of tumor immunotherapy and gene delivery, specifically relating to an aromatic hydrocarbon receptor blocking functional lipid nanoparticle, its preparation method, and its application. The ionizable lipid derived from the aromatic hydrocarbon receptor antagonist has the structure shown in formula (1): Formula (1), where x is an integer between 10 and 16, X is -N(Me)2 or -OH, and n = 0 or 1. This invention designs and synthesizes aromatic ionizable lipids that combine AHR antagonistic activity and nucleic acid delivery capability, constructing a functionalized LNP vector integrating AHR antagonism, nucleic acid delivery, and macrophage targeting. This vector can efficiently transfect macrophages in vivo and express CAR, while simultaneously blocking the AHR pathway in situ to reverse immunosuppression, enhancing antigen presentation, and activating T cell immunity. This fundamentally solves the core problem of the limited efficacy of existing CAR-M in vivo editing technology in solid tumors, especially gliomas.

The present invention relates to novel antibodies and fragments thereof that binds cannabinoid 1 (CB1) receptor. The antibodies and fragments thereof as disclosed herein include humanized antibodies that bind CB1 receptor. The invention also includes uses of the antibodies for treating a disease or disorder responsive to antagonism or agonism of the CB1 receptor.

This invention discloses a traditional Chinese medicine compound for adjuvant chemotherapy in colorectal cancer and its preparation method. The compound is made from the following raw materials in parts by weight: 15-30 parts of Polygonum cuspidatum and 10-20 parts of Citrus aurantium. The preparation method includes: purification treatment, physical primary cell wall disruption, sonic-enzyme synergistic deep cell wall disruption, enzyme inactivation and stabilization, extraction process, concentration process, alcohol precipitation purification, macroporous resin-directed debittering, multi-component complex molecular inclusion, bitter taste receptor antagonism and synergistic taste correction, drying and shaping. This invention's compound, through the precise combination of Polygonum cuspidatum and Citrus aurantium, achieves multi-target synergistic effects, which can reduce the toxic side effects of chemotherapy, enhance the killing effect of chemotherapy on tumors, directly inhibit the proliferation, migration, and invasion of colorectal cancer cells, improve the tumor microenvironment, and reverse chemotherapy resistance. This invention has the advantages of significant chemotherapy synergistic effect, clear toxicity reduction effect, high safety, and wide clinical applicability, and is suitable for adjuvant chemotherapy treatment of colorectal cancer.

The present invention relates to a pharmaceutical composition for oral administration, particularly in the form of a tablet, comprising darolutamide or a pharmaceutically acceptable salt thereof as an active ingredient. Darolutamide is a potent androgen receptor (AR) modulator useful in the treatment of cancer, particularly AR dependent cancer such as prostate cancer, and other diseases where AR antagonism is desired.

The application discloses application of a COL5A3 gene in regulating resistance to vomitoxin and belongs to the technical field of biotechnology. The application constructs a stable and monoclonal COL5A3 gene knockout cell line, and it is found through a vomitoxin toxicity experiment that the COL5A3 gene knockout cell line has excellent resistance to vomitoxin. It is revealed that the COL5A3 gene is a key target point for cells or animals to resist vomitoxin, has important research and application potential for targeted regulation and efficient antagonism of vomitoxin, and based on the gene target point, a targeted drug or vaccine for treating vomitoxin can be developed, thereby providing technical support for food or feed safety.

This invention discloses a compound taste-masking composition for leech decoction, the taste-masking leech decoction, its preparation method, and its application, belonging to the field of traditional Chinese medicine pharmaceutical technology. This invention provides a compound taste-masking composition composed of adenosine monophosphate (AMP), hydroxypropyl-β-cyclodextrin (HP-β-CD), and steviol glycosides, and provides its application method: first, HP-β-CD is added for inclusion and deodorization, then AMP and steviol glycosides are added to synergistically suppress bitterness. This combination utilizes a complementary strategy of "physical inclusion-receptor antagonism-taste neutralization" to simultaneously and efficiently mask the bitterness and fishy taste of leech decoction. Through orthogonal experimental optimization and verification using electronic tongue and sensory evaluation, the optimal formula (AMP 0.10%, HP-β-CD 0.50%, steviol glycosides 0.03%) reduces the bitterness score from 9.3 to 0.6 and the fishy taste score from 9.6 to 1.0. The method of this invention is performed at room temperature and pressure, is simple in process, does not affect the main active ingredients, is suitable for industrial production, and can significantly improve patients' compliance with leech decoction.

The application discloses a kind of second-order multi-agent system consistency control method with noise and counter information, the method comprises: according to the cooperation-antagonism information between second-order nonlinear multi-agent determines the topology structure of second-order nonlinear multi-agent system;Establish the dynamics model of second-order nonlinear multi-agent system;Under the compound noise interference of simultaneously considering additive noise and multiplicative noise, design consistency control protocol;The control protocol is brought into dynamics model, the consistency problem of this multi-agent system is converted into the stability problem of stochastic differential equation, stability analysis is carried out, and position error and speed error are guaranteed to converge.The application designs the consistency control protocol with cooperation-antagonism information under the compound noise interference of simultaneously existing additive noise and multiplicative noise, can greatly improve the anti-interference ability of system, and through stability analysis consistency condition, so that the controlled system is adjusted more easily, reduces control operation complexity.

The application relates to a sensitive information detection and tracing method based on immune confrontation and multi-dimensional fuzzy quantification. The method comprises the following steps: performing deep document structure analysis and adaptive extraction of enhanced optical character recognition on multi-source heterogeneous data respectively to obtain structured data; constructing an anti-sample pool based on an artificial immune mechanism, combining a large language model to construct a sensitive information confrontation detection model, inputting the structured data into the sensitive information confrontation detection model, and outputting a sensitive information result; fusing content sensitivity, influence intensity and source credibility dimensions to perform multi-dimensional fuzzy quantification grading on the sensitive information result; and constructing a directed time sequence graph based on the grading result to perform full-link tracing analysis on high-sensitive information. The method solves the problems of incomplete data extraction, weak confrontation recognition, rough grading and difficult tracing in the prior art, improves the robustness, accuracy and explainability of sensitive information detection, and is suitable for network space sensitive content whole-process management.

The present application belongs to the technical field of analytical chemistry, and particularly relates to a screening method for FcRn small molecule antagonists based on phase transition combined with FRET. In the present application, a fluorescent donor dye required in a FRET process is labeled on IgG, and a fluorescent acceptor dye is labeled on a phase transition material P4VP-SSO3Na-4VP; the phase transition material can reversibly change the phase when the environmental pH changes; when the material changes from a homogeneous system to a heterogeneous system, free IgG in the solution is embedded in the system, the distance between the fluorescent donor and the acceptor in the FRET process is shortened, and the fluorescent signal of the acceptor in the FRET system is detected; and further detection is made on whether the compound has antagonistic effect on FcRn, so as to screen FcRn small molecule antagonists. The present application overcomes the deficiency that some small molecule compounds have no suitable sites for dye labeling; has repeatability, low experimental cost, and can realize high-throughput and rapid screening of FcRn small molecule antagonists.

The application discloses application of Lachnospiraceae bacteria in preparation of a medicine for reducing hepatotoxicity of saikosaponin D, and relates to the field of medicines. The application identifies and applies an intestinal bacteria which has specific antagonism to hepatotoxicity of saikosaponin D for the first time. This breaks the limitation of traditional non-specific regulation through broad-spectrum probiotics or complex compounds, and realizes a leap from'macroscopic flora regulation' to 'key strain targeting'. The strategy directly aims at a key link of SSd toxicity, can effectively protect the liver while retaining the core efficacy of SSd to the greatest extent, and truly achieves the final goal of 'attenuation and efficacy reservation'.