48 results about "Agonist drugs" patented technology

Novel parathyroid hormone (PTH) peptides and analogs thereof of the PTH(1–34) fragment are disclosed that combine the N-terminal signaling domain (residues 1–9) and the C-terminal binding domain (residues 15–31) via a linker. Nucleic acid molecules and peptides for PTH(1–9)-(Gly)5-PTH(15–31) (PG5) and (1–9)-(Gly)7-PTH(15–31) and a novel PTH receptor are disclosed. Additionally, methods of screening for PTH agonists, pharmaceutical compositions and methods of treatment are disclosed.

Disclosed is an extended release pharmaceutical formulation containing at least an alpha-2 adrenergic agonist, such as tizanidine, for the treatment and prevention of spasticity in a subject, e.g., painful inflammatory conditions associated with skeletal muscle spasms.

Provided are pressurized metered dose inhalers containing stable formulations of a beta-agonist drug in suspension or solution. Also provided are aerosol formulations suitable for inhalation therapy containing a beta-agonist drug in suspension or solution.

Compositions and methods for diagnosing neurological disorders such as autism spectrum disorders are disclosed.

The invention provides application of cinnamon oil, cinnamyl aldehyde and derivatives of cinnamyl aldehyde in the preparation of histamine H3 acceptor antagonist or inverse agonist medicaments, and also provides a novel H3 acceptor antagonist or inverse agonist medicament which is formed by using cinnamon oil, cinnamyl aldehyde or derivatives of cinnamyl aldehyde as a main active ingredient and adding other active ingredients. The medicament can be used for preventing and treating senile dementia depression. The H3 acceptor antagonist or inverse agonist medicament provided by the invention has the advantages of clear curing effect, controllable quality and safety, and provides a new choice for clinical work.

The invention specifically discloses new application of salidroside, in particularly application of salidroside to the preparation of a Parkin protein agonist drug. By promoting the expression of parkin protein, salidroside, as a Parkin protein agonist, promotes mitochondrial autophagy and mitochondrial homeostasis, inhibiting apoptosis, and thereby the salidroside can be used for treating the neurodegenerative disease and the degenerative disease of the musculoskeletal system.

The invention relates to the field of biological detection and discloses a detection device and a detection method of a large class of beta-agonists drugs by applying an immune chromatography technology. According to the invention, an antibody/receptor which is reacted with a large class of the beta-agonists drugs is used for preparing an immune chromatography test strip to realize the simultaneous detection of a large class of the beta-agonists drugs. Compared with the prior art, the detection on a large class of the beta-agonists drugs for one time can be realized, the detection cost is low and the method is convenient and fast.

The invention discloses a method for controlling non-invasive brain entry of magnetic nano particles on the basis of a cell drug loading technology. The method comprises a preparation technology of cell (such as red blood cells and neutrophile granulocyte) wrapped magnetic nano particles, a blood brain barrier overcoming technology and a gradient magnetic field positioning and treatment technology. The preparation technology of the cell wrapped magnetic nano particles comprises the steps of hypotonic dilution and isotonic sealing; the blood brain barrier overcoming technology relies mainly onA2a adenosine receptor agonist drugs such as regadenoson; and a gradient magnetic field uses a principle of an electromagnetic effect and is generated by supplying current to a plurality of turns of coils located on an iron core. Magnetic cells of the technology have good magnetism and biocompatibility; accurate targeting and long-time retention of the magnetic cells in a body can be achieved through focusability of the gradient magnetic field; the magnetic nano particles can be positioned in a specific brain area by opening a blood brain barrier; a reaction can be generated in the brain through a pulse magnetic field; and accurate loading of the magnetic nano particles is achieved.

The invention relates to a crystal form C of a long-acting beta2 adrenergic agonist olodaterol hydrochloride and a preparation method thereof and a pharmaceutical composition containing the crystal form C. The crystal form is represented by the characteristic absorption peak of X-ray diffraction pattern. In comparison with the prior art, the crystal form C of olodaterol hydrochloride is not easy to absorb moisture, stability is remarkably raised, and the quality of the product is convenient to control; and the preparation technology is simple, is beneficial to cost control in the industrial production, and has high economic value.

The invention belongs to the field of bio-engineering, and particularly relates to a method for preparing recombinant porcine beta 2-adrenergic receptor protein and an application of the recombinant porcine beta 2-adrenergic receptor protein in rapidly detecting beta 2 agonist medicaments. The recombinant porcine beta 2-adrenergic receptor protein obtained by separation and purification has beta 2 agonist binding activity, SDS-PAGE electrophoresis shows that the molecular weight of the recombinant protein is about 48kDa and the purity of the recombinant protein is more than 80%. The recombinant protein can specifically adsorb beta 2 agonist medicaments and three beta 2 agonist medicaments standard products with different concentrations have an inhibition effect on the reaction when detection is carried out by a competitive ELISA method. According to method disclosed by the invention, the beta 2AR receptor capable of specifically binding with beta 2 agonist is efficiently expressed by a molecular biology method and can be used for rapidly screening beta 2 agonist medicaments instead of conventional antibodies to achieve the detection of multi-residue and screening of unknown substance in medicaments, and the method has good application prospects.

A method for screening a GHSR1a agonist drug mainly comprises the following steps of: 1) carrying out prestimulation for multiple times before administration so as to stabilize basic level of growth hormone; 2) respectively drawing 30 microliters of blood 5, 15, 30, 60, 180 and 300 minutes after administration; 3) separating 10 microliters of blood plasma and using a Rat/Mouse GH ELISA kit to determine the content of the growth hormone in the blood plasma; and 4) choosing a drug, which enables the area rising rate under a blood plasma growth hormone concentration-time curve to be greater than 50%. According to the method for screening the GHSR1a agonist drug, a screening model of the stable, sensitive and repeatable GHSR1a agonist drug is established by the means of assumptive blood collection before administration. The invention can provide a reliable and effective method for screening the GHSR1a agonist drug in animal body.

Optimal ratios of pharmaceutical compositions of beta-1 and beta-2 agonists with their respective antagonists. Safer, more cost-effective drugs for heart and lung therapies are made by combining specific antagonists with their agonists to prevent desensitization of cellular receptors, reducing some of the unwanted side-effects of the agonist drugs alone. Determining the optimal concentration of an antagonist or inhibitor, which is necessary to prevent desensitization, without causing unnecessary and unwanted inhibition, creates a new class of pharmaceuticals. To derive an optimum ratio for a specific composition, a formulative method is provided to detail how competitive antagonists of the receptor should be combined with agonists, in specific proportions, to maximize and maintain receptor response throughout drug administration. The "optimal ratio" methodology used to determine a specific agonist/antagonist composition, to prevent beta-1 or beta-2 receptor desensitization, is experimentally verified and validated for specific compositions. Alteration of a specific ratio is practiced to account for the pharmacokinetic/dynamic differences between animals and humans and within human populations.

Novel parathyroid hormone (PTH) peptides and analogs thereof of the PTH(1-34) fragment are disclosed that combine the N-terminal signaling domain (residues 1-9) and the C-terminal binding domain (residues 15-31) via a linker. Nucleic acid molecules and peptides for PTH(1-9)-(Gly)5-PTH(15-31) (PG5) and PTH(1-9)-(Gly)7-PTH(15-31) and a novel PTH receptor are disclosed. Additionally, methods of screening for PTH agonists, pharmaceutical compositions and methods of treatment are disclosed.

The invention discloses an extraction method and application of an indole monoterpene compound, and belongs to the technical field of traditional Chinese medicine extraction. A pharmacodynamic substance in uncaria rhynchophylla that has a significant agitation effect on a 5-HT1A receptor is clarified, it is found that a compound 1 and a compound 2 have the strong agitation effect on the 5-HT1A receptor. The indole monoterpene compound obtained by extracting can effectively agitate the 5-HT1A receptor, and it is indicated that the compound can be used as an agonist drug for the 5-HT1A receptor.

The invention relates to a crystalline form B of a long-acting beta 2 adrenergic agonist drug olodaterol hydrochloride and a preparation method thereof, and a pharmaceutical composition containing thecrystalline form B, wherein the crystalline form is characterized by an X-ray diffraction pattern characteristic absorption peak thereof. Compared with the prior art, the crystalline form B of olodaterol hydrochloride provided by the invention is not easy to absorb moisture, remarkably improves stability and is convenient for product quality control; the preparation process is simple, which is beneficial to the cost control in industrial production and has high economic value.

The invention discloses a beta-agonist hapten. The molecular structure of the beta-agonist hapten is shown in the following formula (I) in the description. The beta-agonist hapten is successfully synthesized from R-(-)-salbutamol as a raw material by one-step chemical reaction. The hapten is coupled with carrier protein, an artificial antigen is prepared, and the broad-spectrum specific beta-agonist artificial antibody is obtained after immunization. The antibody can recognize 31 kinds of beta-agonist drugs and analogs of the beta-agonist drugs, the semi-inhibitory concentration for R-(-)-salbutamol is 0.5 ng/mL, the linear range is 0.11-40.86 ng/mL, and the minimum detection limit is 0.04 ng/mL. The antibody can detect multiple beta-agonist drugs simultaneously, can be used for on-site rapid detection of food safety and has broad application prospect.

The invention relates to a method for screening an atomization device suitable for a beta2 receptor agonist. The method comprises the following steps: (1) detecting the particle size ratio, the volumeaverage particle size and the surface area average particle size of 1-5[mu]m atomization particles in an atomization device to be screened; (2) detecting the concentration of the electrolyte solution; (3) selecting an atomization device which simultaneously meets the following conditions a) and b): a) the ratio of the particle size of the 1-5[mu]m atomization particles is 50-70%, the ratio of thevolume average particle size to the surface area average particle size is less than and/or equal to 3, and b) the concentration of the electrolyte solution is 0.2-1% w/v.

The invention discloses construction of a GIPR reporter gene stably transfected cell strain, which comprises the following steps: transfecting 293T cells by using CRE reporter gene plasmids, adding eukaryotic antibiotics for screening and monoclonal selection, and performing functional evaluation and selection to obtain an appropriate CRE reporter gene stably transfected cell strain monoclonal; gIPR lentivirus is used for infecting CRE reporter gene stably transfected cell strain monoclonal cells, eukaryotic antibiotics are added for screening and monoclonal selection, and the appropriate GIPR reporter gene stably transfected cell strain is obtained through functional evaluation. A biological activity determination method, a biological analysis quantitative method and a neutralizing antibody determination method which are not limited to GIPR agonist drugs are developed by utilizing the cell strain. The problems that the detection steps are tedious, the time cost is high, the reagent consumable cost is high, experimental data interpretation is complex, the method is not sensitive enough, the anti-interference capacity is poor, the GIPR activation/antagonism mechanism and effect cannot be completely represented, and universality is not achieved are solved.

The invention relates to the field of biological medicine, in particular to a bispecific NK cell agonist as well as a preparation method and application thereof. The invention provides a fusion protein, which takes a CD16A receptor and a 4-1BB receptor as targets to obtain a novel bispecific NK cell agonist drug, namely scfv-CD16A-Trimer-4-1BBL, which has the activity of activating and amplifying NK cells in vitro, enhances the antiviral and anti-tumor capabilities of the NK cells, has potential effects of promoting NK cell proliferation and enhancing T cell functions, and can be used for preparing a novel bispecific NK cell agonist drug. The application potential of in-vitro culture and amplification of the NK cells is achieved, and the amplified NK cells have good cytotoxicity.

A method for treating a patient suffering from neuropathic pain, comprising administering to a patient in need of such treatment an effective amount of an agonist drug capable of binding to the neuronal nicotinic receptor (NNR) but which does not readily cross the blood-brain barrier.

The invention provides a method for broad spectrum identification of beta-receptor stimulant medicines, and relates to the field of medicine testing. According to the method, mass spectrum signals associated with the characteristic chemical structures of the beta-receptor stimulant medicines can be obtained by virtue of an ultra-high-performance liquid chromatography (HPLC)-quadrupole-orbit trap high-resolution mass spectrum device; a characteristic spectrum information base of the beta-receptor stimulant medicines can be built according to the characteristics of mass spectrum signals of the beta-receptor stimulant and the dissociation law of the beta-receptor stimulant. Whether known medicines exist in a sample or not can be identified by comparing high-flux data acquired by the mass spectrum and data in the characteristic spectrum information base; furthermore, whether a novel unknown medicine possibly exists in the sample or not can be predicted by indentifying the modes of the mass spectrum signals; finally, the method for the broad spectrum identification of the beta-receptor stimulant medicines can be formed, so that the beta-receptor stimulant medicines in unknown samples can be rapidly identified. The method provided by the invention has good social benefit and economic benefit.