531 results about "Adrenergic" patented technology

Disclosed is a pharmaceutically-acceptable composition in the form of a solid, amorphous, mono-particulate powder comprising a mixture of:a pharmacologically-effective dosage amount of an adrenergic receptor modulator, or a pharmaceutically-acceptable salt thereof; anda pharmaceutically-acceptable carrier material, which carrier material comprises a maltodextrin with a dextrose equivalent (DE) that is above 15.Compositions are suitable for transmucosal drug delivery, including nasal delivery, by which said compositions may be loaded into a single-use nasal applicator. Compositions are preferably made by way of spray drying and may further include a disaccharide, such as lactose or trehalose which, along with the active ingredient and maltodextrin, may be spray-dried together in combination. Compositions may further comprise one or more alkyl saccharides. Preferred alkyl saccharides include sucrose esters, such as sucrose monolaurate. Preferred adrenergic receptor modulators include epinephrine (adrenaline). The compositions are thus particularly useful in the treatment of allergic reactions, including anaphylaxis.

The inventive subject matter is directed to compositions and methods for ready-to-inject norepinephrine compositions with improved stability. Most preferably, compositions presented herein are substantially antioxidant free and exhibit less than 10% isomerization of R-norepinephrine and exhibit less than 5% degradation of total norepinephrine.

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 medicinal chemistry, and particularly discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. According to the benzimidazole amine derivative disclosed by the invention, R1 is a hydrogen atom or a bromine atom; r2 is substituted benzoyl, substituted benzyl and the like. Pharmacological results show that the benzimidazole amine derivative disclosed by the invention has relatively good antagonistic activity on beta2AR, and the functional activity of isoprenaline (ISO) can be subjected to negative allosteric regulation.

The invention discloses a refining method of a norepinephrine bitartrate intermediate. The refining method of the norepinephrine bitartrate intermediate comprises the following steps: S1, reacting a crude product of the norepinephrine bitartrate intermediate 3 with inorganic acid in an organic solvent to obtain inorganic acid salt of the norepinephrine bitartrate intermediate 3; s2, in the presence of an antioxidant, enabling the inorganic acid salt of the norepinephrine bitartrate intermediate 3 to react with inorganic alkali in water to obtain a refined product of the norepinephrine bitartrate intermediate 3; the structural formula of the norepinephrine bitartrate intermediate 3 is as shown in formula I in the specification. # imgabs0 #

Disclosed in certain embodiments is a method of treating a drug overdose comprising administering to a patient in need thereof a therapeutically effective amount of a respiratory stimulant, wherein the overdosed drug comprises an α2 adrenergic receptor agonist.

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 relates to the technical field of treatment of myopia, and discloses a method and a composition for preventing or treating myopia by adopting vinpocetine, the method comprises vinpocetine, or tropicamide, or phenylephrine hydrochloride, or a combination of these substances as a sole active ingredient for inhibiting or controlling the progression of myopia; the methods in the present application can reduce the dependency of subjects with such visual impairments on corrective lenses. For example, the methods described herein may result in improved vision, including improved visual acuity. Abnormal axial elongation of eyeballs can be avoided, and therefore complications, especially serious retina diseases threatening vision, can be avoided.

The disclosure describes compounds of Formula (I) and Formula (II), which in non-limiting aspects contain an asialoglycoprotein receptor (ASGPR) binding moiety and an anti-β1AR binding moiety. Compounds of Formula (I) and Formula (II) are useful in preventing, treating and / or ameliorating heart failure in a subject when administered therapeutically effective amounts.

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 invention relates to the technical field of cosmetics, and particularly discloses a composition for regulating skin emotion and a preparation method and application thereof. Comprising the following components: aesculus chinensis fruit dry powder, radix sophorae flavescentis dry powder, mint leaf dry powder, geranium leaf dry powder and a solvent. The invention provides a composition for regulating skin mood, which is prepared by compounding dried aesculus chinensis fruit powder, dried radix sophorae flavescentis root powder, dried mint leaf powder and dried geranium leaf powder, and the prepared composition can regulate endogenous'happy hormone 'neurotransmitters (beta-enorphin, cortisol, 5-hydroxytryptamine, noradrenaline and the like) of a human body through skin absorption. Moreover, unhealthy states such as skin sensitivity, tension, redness and swelling, stabbing pain and pruritus caused by mood and pressure problems can be effectively relieved, expression of pressure regulating genes is activated, skin mood is relieved, skin detoxification is promoted, external pollution is defended, oxidation resistance and inflammation diminishing are achieved, and skin is relieved and repaired.

Provided are methods and compositions for treating and / or preventing C. difficile infections, particularly recurring C. difficile infections. The compositions for use in treating and / or preventing C. difficile infections include in some embodiments at least one agent that inhibits an alpha 2 adrenergic receptor, and the presently disclosed methods include administering at least one such composition to a subject in need thereof, optionally in combination with other therapeutically active agents including but not limited to an enhancer of an IL-13 biological activity, optionally an IL-13 peptide or a fragment or homolog thereof; an interleukin-13 receptor subunit alpha-2 (IL-13Ra2) inhibitor; an enhancer of an Interleukin-33 (IL-33) biological activity, optionally an IL-33 polypeptide or a biologically active fragment or homolog thereof; or any combination thereof.

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 present invention describes a composition comprising an effective amount of a combination of two or more components selected from acacetin, ACT1 peptide, α-lipoic acid, alprostadil, anisomycin, apigenin, ascorbic acid, astragalus, berberine, β-lapachone, β-hydroxy-β-methylbutyrate, bacopa monnieri, catechins, catechols, chamomile, chrysin, coumestrol, curcumin, dinitrophenol, dinoprost, ellagic acid, (-)-epigallocatechin gallate, green tea extract, fisetin, genistein, ginsenoside RE, glabridin, 18-α-glycyrrhetinic acid, 18-β-glycyrrhetinic acid, glycyrrhizin, hydroquinone, isoquercetin (EMIQ), shan Phosphate, black bean anthocyanins, leucine, lithium, luteolin, luteolin, luteolin, melatonin, menadione, 1‑methylnicotinamide (MNA), methyl salicylate, myricetin, nicotinamide adenine dinucleotide, nicotinic acid (vitamin B3), nicotinamide (NAM), nicotinamide mononucleotide (NMN), nicotinamide riboside (NR), nicotinic acid adenine dinucleotide (NaAD), nicotinic acid mononucleotide (NaMN), parsley, phenylephrine, pokeweed mitogen, 15‑Δ prostaglandin J2, puromycin, quercetin, quinolinic acid, retinoic acid, trichostatin A, troxerutin, rutin, tryptophan, vitamin D3, withaferin A, wortmannin, and zinc (including its salts).

This invention relates to methods and compositions directed to mobilizing a cell in a subject by blocking CXCR4, a beta-adrenergic receptor, a GPCR, or any combination thereof. In some embodiments, the cell is a hematopoietic stem cell. In some embodiments, the method further comprises administration of G-CSF. This invention also relates to methods of treatment, methods for qualifying a subject for treatment, and methods for preparing a subject for treatment, by blocking CXCR4, a beta-adrenergic receptor, a GPCR, or any combination thereof. In some embodiments, the cell is a hematopoietic stem cell. In some embodiments, the treatment is for cancer. In some embodiments, the CXCR4 is GPC-100. In some embodiments, the method further comprises administration of G-CSF.

The invention belongs to the field of medicinal chemistry, and relates to an indole acrylic acid 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 synthesized compounds, and it is found that the new derivatives can be used as allosteric antagonism regulators of beta2-adrenergic receptors. Trans-indole acrylic acid with different substituent groups is used as a raw material, amide coupling is performed to obtain the novel indole acrylic acid amide derivative, and R1 is a hydrogen atom, a halogen atom, a methyl group or a methoxyl group; r2 is any one of phenyl, m-bromophenyl, m-chlorphenyl, m-fluorophenyl, m-cyanophenyl, m-methoxyphenyl, cyclohexyl and piperidyl. A biological activity test result shows that the indole acrylic acid 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.

The invention discloses a detection method of catecholamine substances and metabolites thereof, freeze-dried powder and application of the freeze-dried powder. The detection method of catecholamine and metabolites thereof comprises the following step: detecting a sample to be detected by adopting a liquid chromatography-tandem mass spectrometry method. According to the present invention, the sample pretreatment and the detection condition optimization are performed so as to achieve the efficient and accurate detection of noradrenaline, epinephrine, variepinephrine, noradrenaline, dopamine and 3-methoxytyramine, the sensitivity is high, the specificity is good, and the new reliable detection method is provided for the detection of catecholamine and metabolites thereof in the blood sample.

The invention relates to the technical field of medical detection, in particular to an endocrine hypertension screening method based on immunological analysis, which comprises the following steps: collecting a random urine sample, removing interferents by using a composite nano adsorbent, and synchronously detecting hormones such as aldosterone, methoxyadrenaline and cortisol and metabolites thereof by using a high-throughput immunity analyzer; integrating detection data based on a dynamic threshold algorithm to generate a screening report, carrying out weighted scoring on positive samples in combination with clinical features, screening high-risk candidate samples, carrying out 24-hour urine retest on the high-risk samples, and if a retest result is still positive, carrying out referral treatment to a specialized department for disease cause definite diagnosis; according to the method, the technical problems of complex sample treatment, low multi-step efficiency and high false positive rate in the prior art are solved, efficient and accurate screening of endocrine hypertension is realized, and reliable support is provided for early diagnosis and targeted treatment.

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 invention discloses a preparation method and application of a mesenchymal stem cell exosome-loaded absorbable suture line, noradrenaline is utilized to activate the surface of a collagen suture line, then human umbilical cord mesenchymal stem cell exosomes are assembled to the surface of the activated suture line through a soaking method, and the absorbable suture line with the surface functionalization is constructed. After the suture line is used, the wound healing effect is good, the blood vessel and cell recovery degree is good, proliferation and migration of fibroblasts can be remarkably promoted, proliferation of T lymphocytes and Th1 cells is effectively inhibited, and a powerful guarantee is provided for tissue repair.

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.

Described herein are methods for the identification and detection of genetic factors in the molecular pathways associated with vascular retinopathies or retinal diseases, for example mild, moderate or severe retinopathy of prematurity (ROP). Included herewith are methods of detecting genetic mutations associated with severe retinopathies, including factors in ADRβ2 pathways, which include RAPGEF3, ADCY7, ADCY9, PRKARIA, and ADCY4 variants. Further, this disclosure provides for methods of treating a subject having a detected genetic factor indicative of ROP.

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 invention relates to a construction method and application of a loneliness mouse model, and the method comprises the steps: placing an experimental mouse in an isolation region in a transparent acrylic isolation cover through an environment in which physical isolation and social deprivation stimulation coexist, forming a visually accessible but physically isolated social environment with five normal living mice, and continuously inducing chronic loneliness for 4 weeks. The effectiveness of the model is verified through a multi-dimensional evaluation system, including behavioristics (open field, elevated maze and three-box experiment), neuroendocrine (serum noradrenaline and angiotensin II), immune inflammatory factors (IL-1beta, IL-6, TNF-alpha and CCL5) and nerve activation (blue spot, almond nucleus, lateral nucleus septum, medial prefrontal cortex and center joint dorsal nucleus C-Fos staining) indexes. According to the intervention method, dynamic environment abundance and social stimulation are adopted, running wheels are arranged, a modular abundance device is arranged, and a social environment of new mice is introduced, so that pathological phenotypes caused by loneliness are reversed. And a systematic experiment tool is provided for exploring association of aloneness and diseases.

The present invention provides a beta-3 adrenergic receptor agonist, along with its pharmaceutical composition, for use in the treatment and / or prevention of pulmonary fibrosis, preferably pulmonary fibrosis associated with bronchopulmonary dysplasia (BPD).

Methods for treating a subject with multiple system atrophy (MSA) using ampleloxetine or a pharma- ceutically acceptable salt thereof are disclosed. The disclosed methods include using ampleloxetine or a pharma- ceutically acceptable salt thereof to (i) treat symptoms of neurogenic orthostatic hypotension in a subject with MSA, (ii) reduce the magnitude of the decline in quality of life in a subject with MSA, and / or (iii) increase the level of norepinephrine in a subject with MSA.

The invention relates to the technical field of primary local hyperhidrosis, in particular to a biomarker for detecting primary local hyperhidrosis and application of the biomarker, and the biomarker comprises but is not limited to one or more of the ratio of Th17 cells to Treg cells, IL-17A, IL-6, ROR gamma t and FoxP3. According to the invention, a multi-dimensional detection system covering PFH core pathological links (immune disorder, hyperactivity of sympathetic nerves and hyperfunction of sweat gland) is constructed by integrating immune related markers such as Th17 / Treg cell ratio, IL-17A, IL-6, ROR [gamma] t, FoxP3 and the like and combining the concentrations of peripheral blood epinephrine (E) and noradrenaline (NE) and the gene expression levels of sweat gland tissues AQP5 and Cacna1c. And a potential molecular target is provided for developing a novel therapeutic strategy (such as specific blocking of an IL-17 signal channel or enhancement of a Treg function) of a targeted Th17 / Treg axis.

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.