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49 results about "Agonist substance" patented technology

An agonist is a drug or an endogenous substance that binds to a Receptor (it has affinity for the receptor binding site) and produces a biological response (it possesses intrinsic activity).

Reagent for quantitative detection of Beta-receptor stimulant through Europium chelate latex time-resolved immunochromatographic assay

Disclosed is a reagent for quantitative detection of a Beta-receptor stimulant through Europium chelate latex time-resolved immunochromatographic assay. The reagent includes test card or test strip which includes a nitrocellulose membrane, absorbent paper, a sample pad and a PVC bottom plate, and a microporous container. A test sample firstly dissolves out Eu3+ fluorescent latex particles which are attached in the microporous container and marked with an anti-Beta-receptor-stimulant small-molecule antibody and after sufficient mixing, the test sample reacts completely with the marker and then a reaction liquid is dropped to the test card or test strip to carry out immunochromatography and at the same time, an immune competition reaction with a Beta-receptor-stimulant small molecule and BSA conjugate which envelopes the nitrocellulose membrane is carried out and five minutes later, the test card or the test strip is inserted into a fluorescent reading meter to measure a fluorescent value so as o obtain a test result. The method is high in sensitivity and quantitative and integrates the advantages of simple and convenient operation and rapidness, the method is applied to rapid detection of veterinary drug residuals such as the Beta-receptor stimulant and the like in food and raw materials on sites of production fields such as plantation, cultivation, animal husbandry and food processing and the like.
Owner:ROHI BIOTECH

Clenobuterol hydrochloride, salbutamol and paylean three joint inspection card and method for processing detecting sample

The invention relates to a clenobuterol hydrochloride, salbutamol and paylean three joint inspection card and a method for processing a detecting sample, and belongs to the technical field of detection of a beta-receptor stimulating agent, wherein a test strip is arranged inside a shell of the three joint inspection card, and the clenobuterol hydrochloride, salbutamol and paylean three joint inspection card is formed by the adhesion of a sample gasket, a colloidal gold membrane, a cellulose nitrate membrane and a water absorbing membrane to a bearing backboard in turn; the colloidal gold membrane is a glass fiber membrane of a colloidal gold marker containing a clenobuterol hydrochloride antibody, a salbutamol antibody and a paylean antibody; three detection strips are arranged on the cellulose nitrate membrane and contain clenobuterol hydrochloride protein conjugate, salbutamol protein conjugate and paylean protein conjugate respectively; and a quality control strip containing an anti-rabbit antibody or an anti-mouse antibody is arranged. The clenobuterol hydrochloride, salbutamol and paylean three joint inspection card has the advantages of simultaneously detecting the clenobuterol hydrochloride, the salbutamol and the paylean in urine or feed, animal tissue, meat and liver. The inspection card is easy to prepare and quick and convenient to use, saves the detection cost, and has accurate result.
Owner:无锡安迪生物工程有限公司

Substituted isoxazole compounds

Disclosed are compounds of Formula (I)or pharmaceutically acceptable salts thereof, whereinQ isR1 is alkyl or aryl, said aryl optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, —OR4, and / or halogen;and R2, R3, R4, and n are defined herein.Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
Owner:BRISTOL MYERS SQUIBB CO

Making method and use of non-human mammal B lymphocyte defect animal model

The invention provides a non-human mammal B lymphocyte defect animal model, a making method of the animal model and a use of the animal model. The Gpr97 gene of the animal model is inactive, so the animal model can be used for researching the biological functions of the Gpr97 gene, and screening or identifying substances capable of increasing the percentage contents of B lymphocytes in the immune system. The invention also provides a use of the G protein coupled receptor 97 protein or a stimulant thereof in the preparation of medicines for increasing the percentage contents of B lymphocytes in the immune system.
Owner:SHANGHAI BIOMODEL ORGANISM SCI & TECH DEV +1

Frovatriptan succinate tablet and preparation method thereof

The invention provides a frovatriptan succinate tablet and a preparation method thereof and belongs to the technical field of medicines. The frovatriptan succinate tablet is mainly prepared from a main drug, filler, a disintegrating agent, a lubricant, a flow aid and a coating material. The frovatriptan succinate tablet is a selective 5HT1 receptor stimulant which is suitable for treating acute attack of migraine with or without aura of an adult. The frovatriptan succinate tablet provided by the invention is safe and effective, stable in quality, low in cost, convenient to administrate, and the patient compliance is enhanced.
Owner:CP PHARMA QINGDAO CO LTD

Novel heteromultimeric ion channel receptor and uses thereof

The present invention describes a heteromultimeric proton-gated ion channel (herein called ASIC-2S.2) with distinctive properties. Compositions and methods are provided for producing and expressing functional ASIC-2S.2 channels, composed of ASIC2A and ASIC3 subunits. The invention also provides genetically engineered expression vectors comprising the nucleic acid sequences encoding both ASIC2A and ASIC3 and host cells coexpressing both ASIC2A and ASIC3 subunits. Also provided herein are genetically engineered nucleic acids encoding chimeric proton-gated ion channels comprised of at least two different subunits, as well as expression vectors and host cells comprising said engineered nucleic acids. The invention also provides for the use of ASIC-2S.2, as well as agonists, antagonists or antibodies specifically binding ASIC-2S.2. in the diagnosis, prevention and treatment of diseases associated with expression of ASIC-2S.2. Also are disclosed methods of influencing electrophysiological, pharmacological and / or functional properties of ASIC-2S.2 as well as methods for screening for substances having ion-channel modulating activity or substances capable of disrupting subunit association or interaction.
Owner:MCGILL UNIV

Centipede analgesic peptide SLP_RhTx and gene and application thereof

The invention discloses centipede analgesic peptide SLP_RhTx and a gene and application thereof. The centipede analgesic peptide SLP_RhTx is composed of an amino acid sequence shown in SEQ ID NO: 1. The gene sequence which encodes the centipede analgesic peptide SLP_RhTx is shown in SEQ ID NO: 2. The centipede analgesic peptide SLP_RhTx is applied as a TRPV1 channel activator to mediate a TRPV1 desensitizing drug. The centipede analgesic peptide SLP_RhTx mediates inactivation of a TRPV1 thermal activated channel by activating TRPV2 to generate analgesic activity for preparing an analgesic drug. The centipede analgesic peptide SLP_RhTx has the advantages that the analgesic peptide can activate and inactivate the TRPV1 channel and specifically inactivate the TRPV2 thermal activated channel so as to generate a powerful analgesic function, and meanwhile, balance of a body temperature adjusting system is not affected. In addition, the analgesic peptide has the characteristics of being simple in structure, convenient to artificially synthesize, quick to respond, strong in analgesic activity and the like, is an excellent candidate medical molecule which takes TRPV1 as an analgesic drug target, and has an important prospect for developing and applying analgesic drugs.
Owner:KUNMING INST OF ZOOLOGY CHINESE ACAD OF SCI

Novel biological substance nesfatin and its related substances and uses thereof

InactiveCN101300346AIncrease hyperactive effectFungiBacteriaThiazolidinedioneAppetite regulation
The present invention relates to a novel method of obtaining a factor involved in appetite control and / or body weight control, as well as genes obtained by said method, polypeptides encoded by said genes, or novel polypeptides obtained from the information on polypeptides encoded by said genes as a means for treating, controlling or diagnosing diseases associated with eating disorders and / or bodyweight control. Also the present invention relates to substances that inhibit the effects of said genes or said polypeptides as a means for treating, controlling or diagnosing diseases associated with appetite control and / or body weight control. By using thiazolidine diones having a PPAR agonist activity, genes and polypeptides involved in appetite regulation and / or body weight reduction can be obtained. NESFATIN or the like obtained by said method can be used as a means for treating, controlling or diagnosing diseases associated with eating disorders and / or body weight control.
Owner:TEIJIN PHARMA CO LTD

Polypeptide compound, preparation, medicine composition, preparation method and application

InactiveCN110790817AGood analgesic activityLow brain permeabilitySenses disorderAntipyreticSide effectStimulant
The invention discloses a polypeptide compound, a preparation, a medicine composition, a preparation method and application. The polypeptide compound has a structural formula as shown in a general formula (I). The polypeptide compound used as a k opioid receptor stimulant has the advantages of better activity, less side effects and better druggability.
Owner:CHENGDU SINTANOVO BIOTECHNOLOGV CO LTD

Aromatic ring compound

InactiveUS20150045378A1Superior GPR4 agonist activityImprove solubilityBiocideSenses disorderDiabetes mellitusMedicinal chemistry
Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I):wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
Owner:TAKEDA PHARMA CO LTD

Protection of normal tissue in cancer treatment

Methods of treating individuals who have cancer are disclosed. In some methods, the cancers may lack functional guanylyl cyclase C and / or p53. In some methods, the methods comprise protecting gastrointestinal cells from genotoxic damage by administering one or more compounds sufficient to elevate intracellular cGMP in the gastrointestinal cells, and then administering chemotherapy and / or radiationtherapy to kill cancer cells. In some methods, the method comprise administering one or more guanylyl cyclase C agonist compounds to intestinal stem cells in the individual an amount of sufficient toactivate guanylyl cyclase C of the intestinal stem cells and elevate intracellular cGMP in the intestinal stem cells, and then administering chemotherapy and / or radiation therapy to kill cancer cells.
Owner:THOMAS JEFFERSON UNIV

Compounds With Mixed Pde-Inhibitory and Beta-Adrenergic Antagonist or Partial Agonist Activity For Treatment of Heart Failure

InactiveUS20080090827A1Increase in ventricular contractilityBiocideSenses disorderRisk strokeMigraine
This invention provides compounds that possess inhibitory activity against β-adrenergic receptors and phosphodiesterase PDE, including phosphodiesterase 3 (PDE3). This invention further provides pharmaceutical compositions comprising such compounds; methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine; and methods of preparing pharmaceutical compositions and compounds that possess inhibitory activity against β-adrenergic receptors and PDE.
Owner:ARTESIAN THERAPECUTICS INC

CANINE iPS CELLS AND METHOD OF PRODUCING SAME

InactiveUS20110033936A1Stable productionEffectively utilizableGenetically modified cellsCell culture active agentsMitogen-Activated Protein Kinase Kinase InhibitorA-DNA
Provided are a method of producing canine iPS cells, comprising (a) the step of bringing into contact with each other a canine somatic cell and a nuclear reprogramming factor, and (b) the step of culturing the cell in a medium containing at least one substance selected from the group consisting of a mitogen-activated protein kinase kinase inhibitor, an activin receptor-like kinase inhibitor, a glycogen synthase kinase inhibitor, a L-type calcium channel agonist and a DNA methylation inhibitor, and a leukemia inhibitory factor, and canine iPS cells that can be obtained by the method.
Owner:KYOTO UNIV

Photo-stimulation method and kit with agonist agent

InactiveUS20130190677A1Increase collagen synthesisReduce inhibitionElectrotherapyMedical devicesIlluminanceMedicine
Disclosed is a photo-stimulation method employing an agonist agent, and a kit for introducing same. The method includes the following steps: providing a light-emitting diode (LED) illuminant which is a yellow, red, green, blue LED or a mixture of two or more kinds thereof, and an agonist agent which contains 0.5% to 2% calcium ion; and adding the agonist agent to a subject and illuminating the subject by the LED illuminant to promote collagen synthesis, to suppress microbial growth, or to inhibit melanin synthesis, wherein the yellow LED is in an illuminance range from 1,000 to 3,500 lux, the red LED is in an illuminance range from 6,000 to 9,500 lux, the green LED is in an illuminance range from 1000 to 5000 lux, and the blue LED is in an illuminance range from 3,000 to 7,000 lux.
Owner:FORWARD ELECTRONICS CO LTD

Analysis method for evaluating in-vitro activity of thrombopoietin receptor stimulant

The invention discloses an analysis method for evaluating in-vitro activity of a thrombopoietin (TPO) receptor stimulant. According to the method, the binding activity of a sample and a TPO receptor and the activity of the thrombopoietin are reflected by evaluating the proliferation-promoting development capacity of the sample on cells. By adopting the method, on one hand, the problem that BaF3-hMpl cell system in the prior art is great in establishing difficulty, great in time consumption and instable in detection result can be solved; on the other hand, the problems that by adopting a suspension cell MTT method, the color developing time is long, an insoluble formazan product is generated, the result reproductivity is poor and the accuracy is low can be solved; meanwhile, a four-parameter data processing method which is better than survival rate evaluation indexes is adopted, so that the activity value of the sample can be directly defined.
Owner:BEIJING TIDE PHARMA

Carrier-free self-assembled nano particle as well as preparation method and application thereof

The invention relates to the technical field of biological medicine, in particular to carrier-free self-assembled nanoparticles as well as a preparation method and an application thereof. The carrier-free self-assembled nano particle is composed of two drug molecules, namely, the photosensitizer and the imidazo quinoline Toll-like receptor stimulant, the preparation method is simple, and the problems that the two hydrophobic drug molecules are poor in water solubility and low in bioavailability are solved at the same time. Compared with other control groups, the photosensitizer chlorin and the Toll-like receptor stimulant nanoparticles (Ce6-IMDQ NPs) show a better in-situ tumor removal effect, and the growth of far-end tumors can be remarkably inhibited through photodynamic-immune combined treatment.
Owner:SHANDONG UNIV

Indole derivatives

The invention relates to indole derivative having the general Formula Iwherein A represents a 5-membered aromatic heterocyclic ring, wherein X1, X2 and X3 are independently selected from N, O, S and CH; Y represents CH2, O, S or SO2; R1 is H, (C1-4)-alkyl, (C1-4)alkyloxy, CN or halogen; R2, R2′, R3, R3′, R4, R4′, R5 and R5′ are independently hydrogen, (C1-4)alkyl (optionally substituted with OH) or CO—OR8; or one pair of geminal substituents R3 and R3′ or R5 and R5′ together represent a keto group, and the others are all hydrogen or (C1-4)alkyl; or R2 and R5 together represent a methylene or an ethylene bridge, and R2′, R3, R3′, R4, R4′ and R5′ are hydrogen; n is 1 or 2; R6 is H, (C1-4)alkyl (optionally substituted with OH, (C1-4)alkyloxy, CO—NR9R10, CO—OR11 or 1,2,4-oxadiazol-3-yl), SO2NR12R13 or COOR14; R7 is H or halogen; R8 is (C1-4)alkyl; R9 and R10 are independently hydrogen, (C1-4)alkyl or (C3-7)cycloalkyl, the alkyl groups being optionally substituted with OH or (C1-4)alkyloxy; R11 is H or (C1-4)alkyl; R12 and R13 are independently H or (C1-4)alkyl; R14 is (C1-6)alkyl; or a pharmaceutically acceptable salt thereof, as agonists of the cannabinoid CB1 receptor, which can be used in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.
Owner:MERCK SHARP & DOHME BV

Novel aminodithioformate compounds, and preparation method and application thereof

The invention discloses novel aminodithioformate compounds, and a preparation method and application thereof, belonging to the field of pharmaceutical chemistry. The structure of the compounds is disclosed as formula I. The research proves that the compounds are PKM2-targeted and are an excitant of PKM2, and also detects that the compounds can generate the antineoplastic action by preventing the PKM2 from entering the karyons. The compounds have favorable antineoplastic action, and have favorable selectivity for tumor cells. Therefore, the compounds can be used as an antineoplastic drug, and have wide application value.
Owner:北京天池凯源科技有限公司

Phenoduopan methanesulphonate medicinal composition and its preparation

InactiveCN100356924CHigh safety for intravenous injectionQuality improvementPowder deliveryLyophilised deliveryFreeze-dryingPharmacometrics
A freeze-dried powder injection of fenoldopam methylsulfonate as the D1-type dopamine receptor excitomotor is prepared from fenoldopam methylsulfonate, the pharmacologically acceptable acidic substance through preparing clear solution and freeze drying.
Owner:CHINA PHARM UNIV

Electrochemical immunosensor as well as preparation method and application thereof

The invention provides an electrochemical immunosensor as well as a preparation method and application thereof. According to the electrochemical immunosensor, Janus particles are prepared by using anaptamer / amino as a functional group and are used for modifying a glassy carbon electrode, thereby preparing the electrochemical immunosensor. The prepared electrochemical immunosensor can be used fordetecting beta-receptor stimulant ractopamine. With the method, the sensitivity and selectivity of the electrochemical immunosensor electrode are improved; the electrode modification process is simpler and more convenient; and the method has high stability and reproducibility and can be applied to detection of ractopamine in human urine.
Owner:SHANXI UNIV

Triazole compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor

InactiveUS8101754B2Organic active ingredientsNervous disorderArylDopamine agonist agent
The invention relates to compounds of the formula I:whereinn is 1 or 2,Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms;R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionially substituted phenyl or 5- or 6-membered heteroaryl;R1a is hydrogen or C1-C4 alkyl; andR2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl;and to the physiologically tolerated acid addition salts of these compounds.The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and / or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
Owner:ABBVIE DEUTSHLAND GMBH & CO KG

Preparation method of P2Y2 receptor stimulant diquafosol tetrasodium

The invention discloses a preparation method of a P2Y2 receptor stimulant, namely diquafosol tetrasodium. The preparation method comprises the following steps: salifying a pyrophosphoric acid compoundas shown in a formula II and long-chain organic amine to obtain a compound as shown in a formula III; activating the compound as shown in the formula III with carbonyl diimidazole to obtain a pyrophosphoric acid active compound as shown in a formula IV; salifying an uridine monophosphate compound as shown in a formula V and long-chain organic amine to obtain a compound as shown in a formula VI; and finally, reacting the compound as shown in the formula IV and the compound as shown in the formula VI in a hydrophilic solvent under the catalysis of Lewis acid to obtain the target product diquafosol tetrasodium as shown in a formula I. According to the method, cation exchange resin is used for treating reaction raw materials which are low in price and easy to obtain and store, organic alkaliand the reaction raw materials are used for salifying to improve thermal stability, and finally, a target product is obtained through anion exchange chromatography purification. The method is efficient, and the produced P2Y2 receptor stimulant is easy to separate and high in yield.
Owner:CHINA PHARM UNIV +1

High-throughput drug screening model using human pregnane X receptor (hPXR)-mediated dual-luciferase reporter gene technique

The invention discloses a high-throughput drug screening model using a human pregnane X receptor (hPXR)-mediated dual-luciferase reporter gene technique. The invention discloses a method for screening a human pregnane X receptor stimulant and an antagonist; by virtue of the method which is a new drug screening method, active drug ligands having regulating effect on a target gene, namely cytochrome CYP450 gene, of the PXR. A human embryonic renal HEK293T cell is subjected to the instantaneous co-transfection of an hPXR expression plasmid, a firefly luciferase reporter gene plasmid and an internal reference renilla luciferase plasmid by virtue of the method. The activities of the firefly luciferase and the renilla luciferase are simultaneously detected to show the regulating effect of the drug on the PXR activity, so as to establish a method for screening the hPXR stimulant and the hPXR antagonist. On one hand, the method can screen out compounds having an hPXR stimulating activity at high throughput from a massive compound library so as to avoid a risk that adverse drugs interact caused by the combined use of new drugs; and on the other hand, the method can screen out compounds having PXR antagonistic activity to inhibit the inducing effect of ligands on drug metabolic enzyme and transporter, so as to reduce the occurrence of adverse DDI and to reverse the drug resistance of anticancer drugs.
Owner:SUN YAT SEN UNIV

Method for measuring the modulation of the activation of a g protein-coupled receptor with gtp analogues

The invention relates to a method for determining the ability of a molecule to modulate the activation of a G protein-coupled receptor (GPCR), said method comprising the following steps:a) introducing, in a first container:a membrane preparation bearing one or more GPCRs and one or more alpha G-proteins,a source of nonhydrolyzable or slowly hydrolyzable GTP labeled with a first member of a pair of RET partners,a ligand of the alpha subunit of a G protein (alpha G-protein) labeled with a second member of the pair of RET partners, said ligand being capable of binding to the full alpha G-protein bound to the nonhydrolyzable or slowly hydrolyzable GTP labeled with the first member of a pair of RET partners,optionally a GPCR agonist;b) measuring the RET signal emitted in the first container;c) introducing (i) in a second container, the same reagents as in step a) and the molecule to be assayed or (ii) in the first container, the molecule to be assayed;d) measuring the RET signal emitted in the second container or in the first container obtained in step c);e) comparing the signals obtained in steps b) and d), a modulation of the signal obtained in step d) relative to that obtained in step b) indicating that the molecule to be tested is capable of modulating the activation of the GPCR.
Owner:CISBIO BIOASSAYS +1

Preparation process of gel composition with sweating function

The invention discloses a preparation process of a gel combination with a sweating function, and relates to the technical field of gels, the technical scheme is as follows: the preparation process comprises preparation of sweating active gel and preparation of conductive solids, and the preparation of the sweating active gel comprises the following specific steps: S1, preparing the conductive solids; the preparation method comprises the following steps: dissolving pilocarpine or nitrate or choline receptor stimulant or organic matter and agar in deionized water according to a certain proportion, heating, stirring to fully dissolve the components after heating, pouring into a gel grinding tool after dissolving, standing, and cooling and solidifying; the preparation process of the gel combination with the sweating function has the beneficial effects that active substances can be excited in a current path to enter a body so as to achieve the sweating function, the gel combination is convenient, can be randomly adjusted, has no side effect on a human body and can be used for a long time, a product can be quickly metabolized by acetylcholine enzyme in the body, and the sweating function is realized. And the method is safe and effective.
Owner:南京子麒舜生物科技有限公司

N-substituted piperidine amide derivative and application thereof

The invention discloses an N-substituted piperidine amide derivative and application thereof and particularly relates to a series of novel N-substituted piperidine amide derivatives and medicine compositions comprising same. The compounds can be used as a 5-HT4 receptor stimulant. The invention further relates to method for preparing the compounds and medicine compositions, and applications thereof in preparing medicines for treating diseases related to 5-HT4 receptor activity, especially medicines for treating irritable bowel syndrome-constipation (IBS-C).
Owner:SUNSHINE LAKE PHARM CO LTD
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