49 results about "Agonist substance" patented technology

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.

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.

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.

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.

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.

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.

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.

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.

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.

Material and method for using 4-1BB agonizes to treat or prevent autoimmune disorders, lymphoproliferative diseases, and allergies are provided.

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.

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.

The invention provides a liquid chromatography-mass spectrometry method for rapidly detecting the content of beta-agonists. The liquid chromatography-mass spectrometry method comprises the following steps: pretreating a sample, namely, sequentially adding water and an organic extracting solution in the sample for extracting a beta-receptor stimulant; then adding a salting-out agent and a water removing agent to ensure that the organic extracting solution and a water phase demix, centrifuging to obtain a first supernate, adding an adsorbing agent in the first supernate for purification, centrifuging to obtain a second supernate, concentrating, re-dissolving and filtering the second supernate to prepare a sample to be detected; and then detecting the beta-receptor stimulant contained in an animal-derived food by adopting an ultra-high performance liquid chromatography-triple quadrupole mass spectrometer. According to the sample pretreatment method suitable for liquid chromatography-mass spectrometry detection, provided by the invention, interfering molecules are removed through extraction and purification so that high accuracy is achieved in sample detection.

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).