301 results about "Adrenergic" patented technology

Intranasal dry powder epinephrine compositions are described herein. The compositions include epinephrine or a pharmaceutically acceptable salt thereof, as well as a stabilizing agent and a carrier. The stabilizing agent is operable to include citric acid, or a pharmaceutically acceptable salt derived therefrom. Such intranasal compositions as described herein are useful in the treatment of health conditions which threaten the central nervous system (CNS) and impede the actions of alpha and beta-adrenergic receptors. Such health conditions include anaphylaxis, bronchospasms, respiratory impairment, organophosphate poisoning, and major adverse cardiac events (MACE).

The invention belongs to the technical field of biological medicines, and particularly relates to application of oxibenzophenone in preparation of a medicine for treating pathological cardiac hypertrophy and / or heart failure. Research results in myocardial cells of primary newborn rats show that Exibenzophenone can inhibit pathological hypertrophy of myocardial cells induced by phenylephrine (PE). Animal experiments show that the epoxybenzophenone can improve cardiac dysfunction induced by aortic arch constriction (TAC) and reduce cardiac hypertrophy and cardiac tissue fibrosis. The invention provides a new drug research and development approach and a drug action target for treating pathological cardiac hypertrophy and heart failure, and has very important medicinal value.

The invention belongs to the field of medicines, and relates to a compound derived from Sinkiang lithospermum, a preparation method thereof and application of the compound in prevention and treatment of cardiovascular diseases. Specifically, the invention discloses a monoterpene benzoquinone derivative with a novel structure in Sinkiang lithospermum, a preparation method of the monoterpene benzoquinone derivative and application of the compound in preparation of anti-myocardial injury drugs. An in-vitro anti-myocardial cell injury activity experiment proves that the compound has a remarkable protection effect on isoprenaline (ISO)-induced H9C2 cell (rat embryo myocardial cell) injury and hypoxia-reoxygenation-induced H9C2 myocardial cell injury. The result shows that the compound can be used for preparing the anti-cardiovascular disease medicine.

The invention belongs to the field of analytical chemistry, relates to material preparation, and particularly discloses a preparation method of a copper-doped covalent organic framework and application of the copper-doped covalent organic framework in adrenaline colorimetric detection. Firstly, 1H-indazole-4, 7-diamine (Iz) and 1, 3, 5-triformyl phloroglucinol (Tp) are used as monomers to synthesize a novel covalent organic framework (Iz-Tp COF) through a Schiff base reaction, copper ions are introduced into the Iz-Tp COF framework to prepare a novel metal covalent organic framework (Iz-Tp (at) Cu), and then according to the phenomenon that the Iz-Tp (at) Cu can catalyze oxidation color development of epinephrine, the metal covalent organic framework (Iz-Tp (at) Cu can catalyze oxidation color development of epinephrine. According to the present invention, the simple, sensitive and efficient adrenaline colorimetric detection method is established, the test conditions are finally optimized, the standard addition method is combined to accurately determine the adrenaline concentration in the urine, and the good practical application value is provided.

The present disclosure provides, among other things, methods, compositions, and uses for treating diseases or disorders characterized by elevated red blood cells using β2 adrenergic receptor antagonists such as β2-specific adrenergic receptor antagonists (e.g., ICI-118551, butaxamine, or pharmaceutically acceptable salts thereof) or β1 / β2-specific adrenergic receptor antagonists (e.g., propranolol or a pharmaceutically acceptable salt thereof). Also provided are methods, compositions, and uses for decreasing erythroid differentiation using the same. Provided methods of treatment comprise administering an effective amount of a β2-specific adrenergic receptor antagonist or a β1 / β2-specific adrenergic receptor antagonist to a patient in need thereof. Also provided are methods, compositions, and uses for ICI-118551 in treating splenomegaly, splenic erythroid hyperplasia, and / or splenic architecture effacement.

The invention belongs to the technical field of microorganisms, and particularly discloses lactobacillus plantarum CX1-3-2 capable of producing gamma-aminobutyric acid and improving sleep and application of the lactobacillus plantarum CX1-3-2. The preservation number of the lactobacillus plantarum CX1-3-2 strain is CGMCC (China General Microbiological Culture Collection Center) No. 34340. The lactobacillus plantarum CX1-3-2 can achieve the effect of improving sleep by improving the levels of GABA and 5-HT in brain tissues and reducing the levels of glutamic acid Glu, dopamine DA and noradrenaline NE; the scavenging rate of DPPH free radicals of the strain reaches 96.4%, the scavenging rate of ABTS free radicals of the strain reaches 78.3%, and the strain has an excellent anti-oxidation effect; the diameters of inhibition zones of the strain on staphylococcus aureus, bacillus cereus, escherichia coli and pseudomonas fluorescens are all larger than 17 mm, and the strain has an excellent antibacterial effect.

The present application relates to novel substituted heterocyclic carboxamides, to processes for their preparation, to their use alone or in combinations for the treatment and / or prevention of diseases and to their use for producing medicaments for the treatment and / or prevention of diseases, in particular for the treatment and / or prevention of breathing difficulties including sleep-induced breathing difficulties such as central and obstructive sleep apnoea, snoring (primary and obstructive snoring), dysphagia, peripheral and cardiac vascular disorders including diabetic microangiopathies and disorders of the peripheral and central nervous system including neurodegenerative and neuroinflammatory disorders.

Methods and compositions are provided for treating individuals exhibiting opioid withdrawal symptoms with opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of opioid withdrawal symptoms, including respiratory depression, sedation, and hypotension. Methods and compositions are also provided for treating stimulant overdose with a benzodiazepine and beta-adrenergic blocking agent. Methods and compositions are also provided for treating concurrent stimulant and opioid overdose comprising administering to a patient in need thereof a benzodiazepine and an opioid antagonist. Methods and compositions are also provided for treating individuals exhibiting opioid withdrawal symptoms or prophy tactically treating individuals for opioid withdrawal symptoms from opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of withdrawal, including respiratory depression, sedation, and hypotension.

The application discloses a preparation method and application of a conjugate targeting pelvic autonomic nerves, wherein the conjugate is NE-RH formed by coupling of rhein and norepinephrine, the conjugate can realize precise targeting of norepinephrine neurons, improve the accumulation effect of RH in the norepinephrine neurons, and further enhance the nerve protection effect of RH. The conjugate has a molecular weight of less than 1000 Da, can help to penetrate the blood-brain barrier, and can avoid the defects of being easily removed by a mononuclear phagocyte system and having a short half-life. The production process of the conjugate is simple, the chemical coupling reaction is clear, the yield can reach 38%, and the purity of the product is greater than 99%, so that the conjugate is convenient to popularize and use. The conjugate and the preparation method have important significance for the damage repair of pelvic autonomic nerves.

The invention belongs to the field of medicinal chemistry, and relates to an indole allylamine amide derivative as well as a preparation method and application thereof. Functional activity screening of G protein dependent signaling pathways is carried out on all the synthesized compounds, and it is found that the new derivatives can be used for preparing beta2-adrenergic receptor allosteric antagonism regulator drugs. Trans-indole allylamine is used as a raw material, amide coupling is performed to obtain the novel indole allylamine amide derivative, and R1 is any one of phenyl, m-methylbenzene, m-methoxyphenyl, m-bromophenyl, m-chlorphenyl, m-fluorophenyl, o-methoxyphenyl, p-methoxyphenyl, naphthalene ring, oxazole, cyclohexyl, cyclopentyl, methyl, ethyl and isopropyl. A biological activity test result shows that the indole allylamine amide derivative disclosed by the invention has relatively good antagonistic activity on beta2AR and can be used for carrying out negative allosteric regulation on the functional activity of isoproterenol.

Intranasal dry powder epinephrine compositions are described herein. The compositions include epinephrine or a pharmaceutically acceptable salt thereof, as well as a stabilizing agent and a carrier. The stabilizing agent is operable to include citric acid, or a pharmaceutically acceptable salt derived therefrom. Such intranasal compositions as described herein are useful in the treatment of health conditions which threaten the central nervous system (CNS) and impede the actions of alpha and beta-adrenergic receptors. Such health conditions include anaphylaxis, bronchospasms, respiratory impairment, organophosphate poisoning, and major adverse cardiac events (MACE).

The invention belongs to the technical field of human body electroencephalogram signal processing and brain regulation and control, and provides a noradrenaline oscillation time-frequency-phase three-dimensional coupling sleep coordinated regulation and control device which comprises the following steps: calculating a three-dimensional coupling coefficient by combining a time domain correlation coefficient, a frequency domain correlation coefficient and an instantaneous phase difference between multi-modal physiological signals; determining the coupling state of the signal based on the three-dimensional coupling coefficient and a preset threshold value; predicting to obtain an optimal regulation factor and a modal weight based on a coupling coefficient matrix constructed based on a time domain correlation coefficient and a frequency domain correlation coefficient and a constructed three-dimensional coupling double-layer optimization architecture in combination with the multi-modal physiological signal; calculating the optimized stimulation intensity in combination with the modal weight, the optimal regulation factor and the multi-modal signal characteristic parameters; and adaptively selecting a stimulation mode and outputting a stimulation signal according to the coupling state of the current multi-mode signal and the optimized stimulation intensity. Accurate matching of stimulation parameters and nerve-blood vessel-cerebrospinal fluid system collaborative rhythm is realized.

Respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) are commonly treated with β2-adrenergic receptor agonists that activate intracellular signaling pathways to induce airway relaxation. However, current therapies are limited by progressive receptor desensitization, or tachyphylaxis, largely attributed to β-arrestin recruitment. This desensitization reduces therapeutic efficacy over time and complicates long-term disease management, resulting in suboptimal outcomes for patients who rely on bronchodilators for daily symptom control. Disclosed herein are pharmaceutical compositions comprising biased agonists and their methods of use, which minimally activate recruitment of beta-arrestin2.

The present invention relates to a compound represented by the following general formula (I) or pharmacologically acceptable salt thereof. The present compound has an excellent adrenergic α1A receptor agonistic action, and is useful as a preventive or therapeutic drug for orthostatic hypotension, essential hypotension, acute hypotension associated with various diseases or conditions, and urinary incontinence.[In the formula, R1 represents a hydrogen atom or a C1-C3 alkyl group; and Z is selected from the group consisting of a substituted phenylamino group, a substituted phenyloxy group, a substituted phenylthio group, a substituted thienylamino group, and the like.]

Compositions and methods for treating neurological conditions are provided. The present invention provides a pharmaceutical composition comprising a dopamine reuptake inhibitor or dopamine agonist, an adrenergic receptor antagonist, and a pharmaceutically acceptable carrier, and a method for treating a neurological disorder by administering the composition.

The present disclosure relates to a method of treatment or prophylaxis of a preterm infant by administering intravenously a therapeutic amount of a composition comprising IGF-1 and IBGBP-3 in combination with a therapy selected from the group comprising: caffeine, fentanyl, fluconazole, gentamicin, insulin, midazolam, morphine, low dose norepinephrine, vancomycin concentrations of 5 mg / ml or less, parenteral nutrition (or a composition for the same use) and combinations thereof.

Pharmaceutical compositions, methods for treating various issues of the eyes, and methods of preparing such compositions are described. These pharmaceutical compositions may be for treating glaucoma, in preparation of eye surgery, during eye surgery, various post-op care (e.g., after cataract surgery, laser eye surgery, and the like), for treating dry eyes, and / or for promoting eyelash growth. These pharmaceutical compositions may comprise such active ingredients (APIs) as: timolol, latanoprost, brimonidine tartrate, dorzolamide, moxifloxacin HCl, dexamethasone PO4, phenylephrine HCl, lidocaine HCl, ketorolac tromethamine, bromfenac, prednisolone PO4, gatifloxacin, amniotic cytokine extract (ACE), prostaglandin E2 (PGE2), and combinations thereof.

A use of intestinal bacteria that co-produce D-lactate and a metabolite thereof D-lactate in predicting exercise capacity. The intestinal bacteria that co-produce D-lactate and the metabolite thereof D-lactate affect the levels of the exercise-related hormones dopamine and adrenaline, thereby significantly impairing exercise capacity. The intestinal bacteria that co-produce D-lactate and the metabolite thereof D-lactate are markers that can be used for routine exercise monitoring and for regulating exercise tolerance.

The application belongs to the field of pharmaceutical chemistry, and specifically discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. In the benzimidazole amine derivative, R1 is a hydrogen atom or a bromine atom; and R2 is a substituted benzoyl group or a substituted benzyl group. Pharmacological results show that the benzimidazole amine derivative has good antagonistic activity on beta2AR and can negatively allosterically regulate the functional activity of isoprenaline (ISO).

The invention relates to a cerebroprotein peptide and casein hydrolysate composition and application thereof in improving sleep and memory, and belongs to the technical field of biological protein peptides. According to the preparation method disclosed by the invention, Maillard modification of the casein enzymolysis primary product is realized by screening the enzymolysis protease of the bovine milk casein and screening the carbonyl compound which is subjected to Maillard reaction with the casein enzymolysis primary product, so that the reducing power, the metal ion chelating capacity and the antioxidant capacity of the casein hydrolysate are effectively improved; furthermore, free radicals in the body are removed, oxidative stress reaction is relieved, and a good foundation is laid for improving sleep quality. The brain protein peptide and the casein hydrolysate are compounded, so that the sleep latency can be effectively shortened, the sleep rate can be increased, the sleep can be effectively improved, the content of dopamine and noradrenaline in hypothalamus can be reduced, the content of 5-hydroxytryptamine and the content of aminobutanoin can be increased, and the brain protein peptide composition has good effects of relieving and treating sleep disorders and improving memory.

There is herein provided a pharmaceutical formulation comprising one or more compounds that are β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, and β3-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, and optionally one or more pharmaceutically acceptable excipient, for use in the treatment or prophylaxis of obesity and other medical uses.

The invention relates to the field of antibodies, in particular to a monoclonal antibody for treating overactive bladder and application of the monoclonal antibody. The monoclonal antibody specifically recognizes and is combined with an adrenergic receptor beta3 (ADR beta3), the monoclonal antibody is obtained through a hybridoma technology, and the M13 monoclonal antibody with high affinity is successfully screened out. The M13 antibody promotes the increase of cAMP concentration in smooth muscle cells and activates a PKA pathway by activating an ADR beta3 receptor, thereby promoting the relaxation of bladder smooth muscles, increasing the bladder capacity and reducing the non-autonomous contraction of detrusor muscles. Animal experiments prove that the M13 monoclonal antibody can effectively improve the urination frequency and urine volume of a mouse OAB model, and has a good clinical application prospect. The monoclonal antibody and the preparation method thereof can be widely applied to the field of treatment of overactive bladder.

Intranasal dry powder epinephrine compositions are described herein. The compositions include epinephrine or a pharmaceutically acceptable salt thereof, as well as a stabilizing agent and a carrier. The stabilizing agent is operable to include citric acid, or a pharmaceutically acceptable salt derived therefrom. Such intranasal compositions as described herein are useful in the treatment of health conditions which threaten the central nervous system (CNS) and impede the actions of alpha and beta-adrenergic receptors. Such health conditions include anaphylaxis, bronchospasms, respiratory impairment, organophosphate poisoning, and major adverse cardiac events (MACE).

The invention relates to application of an alpha1-adrenergic receptor antagonist, in particular to application of the alpha1-adrenergic receptor antagonist in treatment of alopecia, and the alopecia is alopecia caused by abnormal activation of an alpha1-adrenergic receptor. The alpha1-adrenergic receptor antagonist is combined with alpha1-adrenergic receptors of hair follicle cells to reduce the activation degree of the alpha1-adrenergic receptors, and can be used for performing targeted treatment on the alopecia in the rest period caused by abnormal activation of the alpha1-adrenergic receptors. A new action target is provided for treatment of alopecia in the stationary period.

The application relates to a reagent combination for detecting depression, a manufacturing method, a detection system and application thereof, and belongs to the technical field of instrument detection. The reagent combination for detecting depression comprises a calibrator, a quality control sample and an extraction solution of a to-be-detected compound serving as a biomarker; wherein the to-be-detected compound is at least three kinds selected from 5-hydroxyanthranilic acid, methionine, gamma-aminobutyric acid, 3,4-dihydroxyphenylacetic acid, 2-picolinic acid, quinolinic acid, kynurenine, 5-hydroxytryptamine, 3-hydroxykynurenine, 3-hydroxyanthranilic acid, dopamine and norepinephrine. The reagent combination for detecting depression and the detection system can significantly improve the accuracy of diagnosis, are convenient to detect, have good repeatability of detection data, are high in specificity, and are accurate in clinical diagnosis results.

There is provided herein a β2-adrenergic receptor agonist, or a pharmaceutically acceptable salt thereof, for use in the treatment and / or prophylaxis of hyperglycaemia or a disorder characterized by hyperglycaemia, wherein the treatment and / or prophylaxis further comprises administration of an SGLT2 inhibitor.

The invention discloses an epinephrine drug nitrosamine impurity as well as a preparation method and application thereof. According to the method, an epinephrine drug is taken as a raw material, hydroxyl is protected through a silane protecting group, the protected hydroxyl and a nitrosation reagent are subjected to a selective nitrosation reaction, and then the target nitrosamine impurity is obtained through a deprotection reaction. According to the method, the high-purity nitrosamine impurity of the epinephrine medicine can be prepared and used as a reference substance for qualitative and content detection of the nitrosamine impurity in the production process of raw materials and medicines, so that it is ensured that the epinephrine raw material medicine and preparations meet the medicinal standard; the method has important significance in improving the quality of epinephrine drugs and guaranteeing the medication safety.

In various aspects and embodiments provided are compositions and methods for identifying patients in need of improving cognition and / or treating a neurodegenerative disease in a patient and treating such patient. More specifically, the disclosure in some embodiments includes administration of a β-AR agonist and a peripherally acting β-blocker (PABRA) to a patient in need thereof.

Intranasal dry powder epinephrine compositions are described herein. The compositions include epinephrine or a pharmaceutically acceptable salt thereof, as well as a stabilizing agent and a carrier. The stabilizing agent is operable to include citric acid, or a pharmaceutically acceptable salt derived therefrom. Such intranasal compositions as described herein are useful in the treatment of health conditions which threaten the central nervous system (CNS) and impede the actions of alpha and beta-adrenergic receptors. Such health conditions include anaphylaxis, bronchospasms, respiratory impairment, organophosphate poisoning, and major adverse cardiac events (MACE).

Intranasal dry powder epinephrine compositions are described herein. The compositions include epinephrine or a pharmaceutically acceptable salt thereof, as well as a stabilizing agent and a carrier. The stabilizing agent is operable to include citric acid, or a pharmaceutically acceptable salt derived therefrom. Such intranasal compositions as described herein are useful in the treatment of health conditions which threaten the central nervous system (CNS) and impede the actions of alpha and beta-adrenergic receptors. Such health conditions include anaphylaxis, bronchospasms, respiratory impairment, organophosphate poisoning, and major adverse cardiac events (MACE).