65 results about "Adenosine A1 receptor" patented technology

A composition and various formulations comprise preventative or therapeutic amounts of an epiandrosterone, analogue thereof or salt thereof, and / or a ubiquinone or salt thereof, and a pharmaceutically or veterinarily acceptable carrier or diluent. The composition and formulations are useful for treating bronchoconstriction, respiratory tract inflammation and allergies, asthma, and cancer. A method of treating diseases associated with low adenosine levels or adenosine depletion comprises administering folinic acid or a pharmaceutically acceptable salt hereof in a preventative or therapeutic amount, or an amount effective to treat adenosine depletion.

The invention provides methods and compositions for reducing or inhibiting bone resorption, osteoclast differentiation and stimulation and the loosening of medical prostheses by administering a compound or agent that modulates an adenosine receptor such as the adenosine A2A receptor, in particular, an agonist of an adenosine A2A receptor. The invention also extends to pharmaceutical compositions comprising such an agent that modulates an adenosine receptor such as an adenosine A2A agonist and to prosthetic devices containing such an agent that modulates an adenosine receptor such as an A2A agonist on one or more surfaces or within the prosthetic device such as, for example, suspended in the cement forming the prosthetic device.

Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.

This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.

Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment of toxic side effects of a drug or prevention or treatment of leukopenia, particularly drug-induced leukopenias; and inhibition of abnormal cell growth and proliferation.

The present invention relates to pharmaceutical compositions for use in inducing proliferation of the hematopoietic system, in particular, of bone marrow cells, comprising a pharmaceutically acceptable carrier, excipient or diluent and, as an active ingredient, an effective amount of an adenosine A1 receptor agonist. The pharmaceutical composition of the present invention may be used to induce proliferation of bone marrow cells, in a variety of clinical situations where such proliferation is therapeutically beneficial.The active ingredient within the pharmaceutical composition of the invention may be a compound of general formula (I) as described herein or any other compound or substance which specifically binds to and / or activates the A1 adenosine receptor and acts as an agonist to the receptor's natural ligand.

The present invention relates to compositions and methods for modulating melanin production, secretion and / or accumulation in human skin cells. In particular, the present invention relates to the use of A3 adenosine receptor antagonists in compositions and methods for the treatment and amelioration of hyper-pigmentation conditions and for the lightening of skin, and to the use of A3 adenosine receptor agonists in compositions and methods for the treatment and amelioration of hypo-pigmentation conditions and for the tanning of skin.

This invention provides a method of mitigating / ameliorating one or more components of addictive behavior associated with chronic consumption of a substance of abuse, or withdrawal therefrom. The method typically involves administering to a subject in need thereof an adenosine A2A receptor antagonist in an amount sufficient to ameliorate said one or more components of addictive behavior.

Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V):as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.

The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

The invention provides methods and compositions for modulating osteoclastogenesis and for treating bone diseases characterized by bone loss or a decrease in bone mass or density, by administering a compound or agent that modulates the adenosine A1 receptor, in particular, an inhibitor or antagonist of the A1 receptor.

The present invention concerns methods and reagents useful in modulating adenosine A1 receptor (ADORA1) gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to small interfering RNA (siRNA) molecules capable of mediating RNA interference (RNAi) against ADORA1 and related receptors.

The present invention relates to a method of increasing blood brain barrier (“BBB”) permeability in a subject. This method involves administering to the subject an agent or agents which activate both of the A1 and A2A adenosine receptors. Also disclosed is a method to decrease BBB permeability in a subject. This method includes administering to the subject an agent which inhibits or blocks the A2A adenosine receptor signaling. Compositions relating to the same are also disclosed.

The present invention relates to the use of adenosine type 3 receptor (A3R) modulators to modulate serotonin transporter (SERT) function in vivo. In particular, antagonists of A3R can be used to inhibit A3R-dependent upregulation of SERT, for example, as antidepressants.

The present invention relates to method for treating inflammatory bowel disease that includes administration of an effective amount of an antagonist of A2B adenosine receptors (ARs).

The invention relates to an application HEA of N (6)-(2-hydroxyethyl)-adenosine (HEA) and derivatives thereof in medicine or food preparation as an adenosine A1 receptor stimulating agent as well as an application of the derivatives thereof in treating nervous system diseases, such as calming and hypnotizing, anti-convulsion, cerebral protection, Parkinson disease, drug addiction and the like, related to an adenosine receptor conditioner. The invention offers a new drug source for the prevention of nervous system diseases.

Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.

The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, an ischemic condition, a reperfusion injury, obesity, a wasting disease, or diabetes, comprising administering an effective amount of a Purine Derivative to an animal in need thereof.

The present invention provides a method for identifying parital adenosine A1 receptor agonists that are useful in the treatment of arrhythmias. Partial adenosine A1 receptor agonists and methods for using partial adenosine A1 receptor agonists to treat arrhythmias in mammals.

The present disclosure provides compounds useful in the amelioration, prevention or treatment of A3 adenosine receptor mediated diseases, such as glaucoma and glaucoma-related ocular disorders, having the structure of Formula I as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for ameliorating, preventing or treating A3 adenosine receptor mediated diseases using the compound.

This invention pertains to compounds which specifically inhibit the adenosine A1 receptor and the use of these compounds to treat a disease associated with A1 adenosine receptors in a subject.

This compounds correspond to the formula (I), where: R1 represents and aryl or heteroaryl group optionally substituted by one or more substituents selected from the group consisting of halogen atoms, straight or branched optionally substituted lower alkyl, cycloalkyl, hydroxy, straight or branched, optionally substituted lower alkoxy, cyano, or -CO2R', wherein R' represents a hydrogen atom or a straight or branched, optionally substituted lower alkyl group; R2 represents a group selected from: a) a straight or branched lower alkyl group substituted by one or more carboxylic groups (-COOH) andoptionally substituted by one or more halogen atoms; b) a cycloalkyl group substituted by one or more carboxylic groups (-COOH) and optionally substituted by one or more halogen atoms; c) a straight or branched alkylcycloalkyl or cycloalkylalkyl group substituted by one or more carboxylic groups (-COOH) and optionally substituted by one or more halogen atoms.

The invention discloses a small-molecular antagonist for an A3 adenosine receptor, and an application thereof in medicine synthesis, and concretely relates to a use of the small-molecular antagonist for the A3 adenosine receptor and pharmacologically available salts of the small-molecular antagonist for the A3 adenosine receptor as medicines for treating or preventing A3 adenosine receptor-mediated related diseases or symptoms.

The invention provides a cordycepin-containing composition, and belongs to the field of traditional Chinese medicine preparations. The cordycepin-containing composition is prepared from the followingraw materials in parts by weight: 0.1 to 3 parts of cordycepin and 1 to 12 parts of nuciferine. The cordycepin-containing composition provided by the invention is simple in compatibility, the source of raw materials is wide, accumulation of white fat and the contents of serum TC (Total Cholesterol), TG (Triglyceride) and LDL (Low-Density Lipoprotein) can be remarkably reduced, the content of HDL (High-Density Lipoprotein) can be remarkably increased, the protein level of a adenosine A1 receptor of a GH3 cell can be induced to be increased, and lactation release of the GH3 cell can be remarkably inhibited; visually, the cordycepin-containing composition provided by the invention is capable of preventing obesity, losing weight, preventing / treating hyperlipidemia, conditioning lipoprotein abnormality, conditioning lipid metabolism and reducing an occurrence rate of a coronary heart disease at the same time.

Provided are therapeutic and / or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and / or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.

The present invention relates to a method for inducing proliferation of the hematopoietic system, in particular, of bone marrow cells, comprising administering to a subject an effective amount of an adenosine A1 receptor agonist. The method of the invention may be utilized n a variety of clinical situations where such proliferation is therapeutically beneficial. The active ingredient within the pharmaceutical composition of the invention may be a compound of general formula (I) as described herein, or any other compound or substance which specifically binds to and / or activates the A1 adenosine receptor and acts as an agonist to the receptor's natural ligand.

The present invention relates to a method of inducing proliferation of bone marrow cells in a subject, compromising administering to the subject an effective amount of an adenosine A1 receptor agonist. The present invention further relates to a method for preventing reduction in level of leukocytes in a subject as a result of a treatment comprising administering to the individual an effective amount of an adenosine A1 receptor agonist. In addition, the invention relates to a method of treatment of an individual comprising administering to the subject a therapeutic drug in combination with an adenosine A1 receptor agonist.

The invention relates to construction and application of adenosine 5'-monophosphate mediated nano transmission system for a target tumor and discloses novel compound adenosine 5'-monophosphate capable of targeting tumor cells. The compound plays the targeting role by identifying adenosine A1 receptors expressed on the surfaces of the tumor cells, can be connected with a few detectable markers such as fluorescent marks for preparation of a targeting tumor diagnosis preparation and can also be connected with a few substances with tumor inhibition activity for preparation of a targeting tumor inhibition preparation.