57 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).

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).

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 involve treating atrial fibrillation with bucetinol after determining that the patient, including the patient with heart failure, is homozygous for Arg389 in the β1-adrenergic receptor gene.

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 present invention relates to compounds that are activators of the Alpha1A-Adrenergic Receptor (α1A-AR) and methods of using such compounds: for treating neurological conditions, for cardio-protection, and for treating other conditions. In certain embodiments, the α1A-AR activator compound is a compound of Formula I. In certain embodiments, the neurological condition is Alzheimer's disease, benign prostatic hyperplasia, memory loss, depression, or Parkinson's disease.

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 disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor. In certain embodiments of the methods disclosed herein, the methods include administering to the subject a compound as disclosed herein and a peripherally acting P-blocker (PABRA).

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)

The present invention discloses an immunogenic peptide segment for human β1-adrenergic receptor and its application, wherein the amino acid sequence of the immunogenic peptide segment is DEARRCYND, as shown in SEQ ID NO.1. The immunogenic vector vaccine for human β1-adrenergic receptor is prepared by coupling the above-mentioned immunogenic peptide segment of human β1-adrenergic receptor with a carrier, and the carrier is Qβ-2aa bacteriophage virus-like particle protein. The present invention successfully couples the preferentially designed immunogenic peptide segment of human β1-adrenergic receptor with the Qβ-2aa bacteriophage virus-like particle protein carrier to prepare a vector vaccine. The immunogenic vector vaccine can be used to prepare drugs for treating hypertension and improving cardiac remodeling after myocardial infarction.

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 purpose of the present invention is to provide a method for evaluating a drug using myocardial cells and with which it is possible to stably evaluate the effect of a drug such as a muscarinic receptor agonist, an adrenergic receptor inhibitor, and a muscarinic receptor inhibitor on the heart rate. And a reagent and a kit for performing the method for evaluating the drug. According to the present invention, provided is a method for evaluating a drug, comprising: a step for treating myocardial cells with a culture medium containing a physiologically active substance of the sympathetic nervous system and / or a physiologically active substance of the parasympathetic nervous system; a step in which a drug is brought into contact with the treated myocardial cells; and evaluating the influence of the drug on the heart rate of the myocardial cells.

The present invention belongs to the field of medicinal chemistry, and particularly relates to the use of a phenylalanine amide derivative as an allosteric antagonist of the β2-adrenergic receptor. The structural formula of the phenylalanine amide derivative is shown in Formula 1 and Formula 2. The pharmacological results show that most of the target compounds synthesized in the present invention have antagonistic activity against β2AR and can negatively allosterically regulate the functional activity of isoproterenol.

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.

The present invention belongs to the field of medicinal chemistry and relates to the application of N-substituted benzylpyrazole derivatives as allosteric modulators, antagonists, and agonists of the β2-adrenergic receptor. The present invention uses acetophenone or acetophenone with different substituents as raw materials, undergoes a Claisen condensation reaction, cyclization, and then substitution and hydrolysis reactions, followed by an amide coupling reaction to finally obtain a series of new pyrazole derivatives with the structure shown in formula (1), where R1 is a hydrogen atom, a halogen atom, a nitro group, or a methoxy group; R2 is a hydrogen atom, a halogen atom, a cyano group, a nitro group, or a methoxy group; and R3 is a halogen atom. Functional activity screening of the G protein-dependent signaling pathway was performed on all synthesized compounds, and it was found that these new derivatives can act as agonists, positive allosteric modulators (PAMs), antagonists, and negative allosteric modulators (NAMs) of the β2-adrenergic receptor. #imgabs0#

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).