47 results about "Adrenergic receptor" 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 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.

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 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).

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).

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 current methods and compositions relate, in certain aspects, to treatment of atrial fibrillation with bucindolol in patients, including patients with heart failure, after being determined to have non-internalizing ß-adrenergic receptors.

The invention belongs to the field of pharmaceutics, particularly relates to a composition containing levosalbutamol hydrochloride and ipratropium bromide as well as a preparation method and application of the composition, and overcomes the defects of a stabilizer disodium ethylene diamine tetraacetate adopted in the prior art. The invention provides a levosalbutamol hydrochloride and ipratropium bromide composition which is simpler in prescription and better in safety, can be used for treating reversible bronchospasm related to airway obstructive diseases, can jointly act on muscarinic acid and beta2 adrenergic receptors in the lung, can enhance the bronchiectasia effect, takes effect quickly, and is free of toxic and side effects. The clinical application value is very high.

The present invention relates to a plurality of engineered variants based on muscarinic toxin MT3 which specifically bind to muscarinic acetylcholine receptor M4 or adrenergic receptor alpha 2A, preferably human muscarinic acetylcholine receptor M4 or human adrenergic receptor alpha 2A.

An object of the present invention is to provide a drug evaluation method using myocardial cells, which can stably evaluate an effect of a drug such as a muscarinic receptor agonist, an adrenergic receptor inhibitor or a muscarinic receptor inhibitor on a heart rate; and a reagent and a kit for carrying out the drug evaluation method. According to the present invention, there is provided a drug evaluation method including: treating myocardial cells with a culture medium containing a physiologically active substance of a sympathetic nervous system and / or a physiologically active substance of a parasympathetic nervous system; bringing a drug into contact with the myocardial cells treated as above; and evaluating an effect of the drug on a heart rate of the myocardial cells.

The present invention relates to novel compounds of formula I or any pharmaceutically acceptable salt, crystal, stereoisomer, hydrate, solvate, prodrug, metabolite or solvate thereof. Among other properties, the compounds of the invention exhibit long-acting muscarinic antagonism (LAMA) or dual pharmacological activity at the muscarinic M3 receptor and the beta-2 adrenergic receptor (MABA), which are useful for the treatment of respiratory conditions, such as asthma, chronic obstructive pulmonary disease (COPD) and rhinitis for example. The invention encompasses the compounds, reagent and intermediate compounds, processes for obtaining the compounds of the invention, pharmaceutical compositions, combinations and medicaments containing them and their therapeutic uses and methods for the treatment of human diseases in which such receptors are involved. formula (I)

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 the therapeutic application of multifunctional compounds that act as α2 adrenoreceptor antagonists and cholinesterase inhibitors for the treatment of Alzheimer's disease and other neurodegenerative diseases, or the concomitant use of a mixture of an α2 adrenoreceptor antagonist and a cholinesterase inhibitor to achieve the same effect.

The invention discloses a cell model for simulating acute pressure alopecia as well as a construction method and application thereof, the construction method comprises the following steps: A, culturing primary hair papilla cells obtained by separation, and performing passage; and B, stimulating the passage cells for 24-72 hours by using an adrenergic receptor beta agonist, and then measuring the cell activity and the expression quantity of an alopecia-related gene DKK1, thereby obtaining the cell model for simulating acute stress alopecia. The adrenergic receptor beta agonist is used for inducing the hair papilla cells, and the obtained hair papilla cell model can simulate the physiological characteristics of the hair papilla cells of people under acute pressure; based on the model, a substance used for preventing and / or relieving acute pressure alopecia or used for evaluating the anti-alopecia effect of a to-be-detected substance on acute pressure alopecia can be further screened out, and a new solution is provided for developing products or methods for preventing and / or relieving acute pressure alopecia and promoting hair regeneration under pressure.

The present invention relates to novel compounds of formula I or any pharmaceutically acceptable salt, crystal, stereoisomer, hydrate, solvate, prodrug, metabolite or solvate thereof. Among other properties, the compounds of the invention exhibit long-acting muscarinic antagonism (LAMA) or dual pharmacological activity at the muscarinic M3 receptor and the beta-2 adrenergic receptor (MABA), which are useful for the treatment of respiratory conditions, such as asthma, chronic obstructive pulmonary disease (COPD) and rhinitis for example. The invention encompasses the compounds, reagent and intermediate compounds, processes for obtaining the compounds of the invention, pharmaceutical compositions, combinations and medicaments containing them and their therapeutic uses and methods for the treatment of human diseases in which such receptors are involved.

The application discloses a preparation process of effervescent granules of a composition containing phenylephrine hydrochloride, which is prepared by taking phenylephrine hydrochloride as a main active ingredient, and by adding antiallergic agents, expectorants, antitussives, antipyretics, anti-inflammatory agents and combinations thereof. In order to prevent degradation of phenylephrine hydrochloride, the phenylephrine hydrochloride is first wrapped with PEG together with an alkali source, and then mixed with other components to prepare the effervescent granules. The effervescent granules prepared by the method have the advantages of high drug stability, rapid effect, high bioavailability, convenient carrying and low cost, and are suitable for children, the elderly and patients who cannot swallow solid preparations.

The present disclosure provides compositions that provide positive allosteric modulator compounds of the beta-adrenergic receptor in combination with a beta-arrestin-biased beta-blocker, such as carvedilol, for the treatment of cardiovascular diseases and disorders, such as hypertension and heart failure, wherein the effectiveness of the beta-blocker is enhanced by positively augmenting carvedilol-stimulated cellular responses.

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 imped the actions of alpha and beta-adrenergic receptors. Such health conditions include anaphylaxis, bronchospasms, respiratory impairment, organophosphate poisoning, and major adverse cardiac events (MACE).

Described herein, inter alia, are 0.2 A adrenergic receptor agonists and uses thereof.

This invention belongs to the field of medicinal chemistry, specifically disclosing a pyrrolamide derivative, its preparation method, and its application as an allosteric antagonist of the β2-adrenergic receptor. The pyrrolamide derivative of this invention has the structure shown in Formula I, wherein R1 is ethyl, methyl, isopropyl, etc.; and R2 is a fatty amine, aniline, m-bromoaniline, benzylamine, etc. Pharmacological results show that the pyrrolamide derivative of this invention has good antagonistic activity against β2AR and can negatively allosterically regulate the functional activity of the ortho-agonist β2AR agonist isoproterenol (ISO).

To provide a pharmaceutical composition having enhanced active ingredient permeation characteristics.SOLUTION: The pharmaceutical composition comprises a polymer matrix, a pharmaceutically active ingredient comprising epinephrine or a prodrug thereof in the polymer matrix, and an adrenergic receptor interacting substance. Preferably, the pharmaceutical composition further comprises a permeation enhancer, and preferably, the pharmaceutical composition is a film further comprising a polymer matrix, and the pharmaceutically active ingredient is contained in the polymer matrix.SELECTED DRAWING: Figure 1A

The present invention relates to a method and composition for mobilizing cells from a subject by blocking CXCR4, beta-adrenergic receptors, GPCRs, or any combination thereof. In some embodiments, the cells are hematopoietic stem cells. In some embodiments, the method further comprises the administration of G-CSF. The present invention also relates to a treatment method, a method for qualifying a subject for treatment, and a method for preparing a subject for treatment by blocking CXCR4, beta-adrenergic receptors, GPCRs, or any combination thereof. In some embodiments, the cells are hematopoietic stem cells. In some embodiments, the treatment is for cancer. In some embodiments, CXCR4 is GPC-100. In some embodiments, the method further comprises the administration of G-CSF.

The invention discloses a humanized monoclonal antibody of a beta1-adrenergic receptor as well as a kit and application of the humanized monoclonal antibody. The amino acid sequence of the humanized monoclonal antibody of the beta1-adrenergic receptor is as shown in SEQ ID No.1. The invention further discloses a preparation method of the humanized monoclonal antibody of the beta1-adrenergic receptor. According to the distribution condition of myocardial antigenic determinants, polypeptides of natural antigenic determinants are designed and synthesized to immunize animals to prepare monoclonal antibodies and carry out humanized expression, so that the antibody detection kit is prepared. The kit can be used for auxiliary diagnosis of autoimmune response activation and prognosis judgment of patients with viral myocarditis and dilated cardiomyopathy, and auxiliary establishment of a patient treatment scheme.

The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor.

The current methods and compositions relate to treatment of atrial fibrillation with bucindolol in patients, including patients with heart failure, after being determined to be homozygous Arg389 in the β1 adrenergic receptor gene.

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).

Yohimbine derivatives, their preparation methods, and uses. This invention discloses compounds of Formula I and pharmaceutical compositions comprising compounds of Formula I. The compounds of Formula I of this invention, as adrenaline receptor α2A (ADRA2A) antagonists or partial antagonists, can treat and / or prevent inflammatory bowel disease (IBD), particularly ulcerative colitis (UC), Crohn's disease (CD), or enteritis.