Search Results - antagonists

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Novel Dopamine D2 Receptor Antagonists and Methods of Their Use

Investigators at the NIH have identified a series of novel, small molecule antagonists of the dopamine D2 receptor. Among the dopamine receptor (DAR) subtypes, D2 DAR is arguably one of the most validated drug targets in neurology and psychiatry. For instance, all receptor-based anti-Parkinsonian drugs work via stimulating the D2 DAR, whereas all FDA...

Published: 7/25/2024 | Inventor(s): Juan Marugan, Jingbo Xiao, Marc Ferrer-Alegre, Noel Southall, R Benjamin Free, David Sibley

Keywords(s): Agents, ANTAGONISTS, ANTIPSYCHOTIC, D2, Dopamine, Human, NB2BXX, NB2XXX, Potential, RECEPTOR, SELECTIVE, VEXXXX, VNXXXX, WIXXXX, WKXXXX, YBXXXX, YCXXXX

Category(s): Collaboration Sought > Collaboration, TherapeuticArea > Psychiatry/Mental Health, TherapeuticArea > Neurology, Application > Research Materials, Application > Therapeutics

Small Molecule MRS5474 with Anticonvulsant Activity for Treatment of Epilepsy

Adenosine modulates many physiological processes by activating specific adenosine receptors. These adenosine receptors play a critical role in the regulation of cellular signaling and are broadly distributed throughout the body. Thus, the ability to modulate adenosine receptor-mediated signaling is an attractive therapeutic strategy for a broad range...

Published: 7/25/2024 | Inventor(s): Dilip Tosh, Kenneth Jacobson

Keywords(s): A3, Activity, ADENOSINE, AGONISTS, Agonists:, Al, ANTAGONISTS, Anticonvulsant, Derivatives, Docking, IB1FXX, IB1XXX, IBXXXX, IXXXXX, NB1EXX, NB1HXX, NB1XXX, NBXXXX, N-Methanocarba, Nucleosides, NXXXXX, PARTIAL, Patent Category - Chemistry, POTENT, RECEPTOR, TRUNCATED

Category(s): Collaboration Sought > Collaboration, TherapeuticArea > Neurology, Application > Diagnostics, Application > Research Materials, TherapeuticArea > Cardiology, Application > Therapeutics

Antagonists of Hyaluronan Signaling for Treatment of Airway Diseases

Airway diseases, such as Asthma and Chronic Obstructive Pulmonary Disease (COPD), constitute a major health burden worldwide. It is estimated, for example, that nearly 15.0% of the adult population in the US are affected with such diseases, and the economic cost burden is over $23 billion annually. Unfortunately, the current options for treatment of...

Published: 7/25/2024 | Inventor(s): John Hollingsworth, Bryan Toole, Jian Liu, Stavros Garantziotis

Keywords(s): AIRWAY, ANTAGONISTS, hyaluronan, Hyperresponsiveness, IB4XXX, IBXXXX, Inflammation, IXXXXX, SIGNALING, treatment, VPXXXX, WKXXXX, YBXXXX, YCXXXX

Category(s): Collaboration Sought > Collaboration, TherapeuticArea > Ophthalmology, Application > Therapeutics, TherapeuticArea > Endocrinology, TherapeuticArea > Oncology, TherapeuticArea > Dental, Application > Diagnostics, Application > Research Materials, TherapeuticArea > Cardiology, TherapeuticArea > Infectious Disease, TherapeuticArea > Pulmonology

Antagonist of A3 Adenosine Receptor Fluorescent Probes for the Study of Diseases that Involve A3 Signaling

This molecular probe may serve as a companion tool to identify and stratify patient populations based on the prevalence of the target A3 adenosine receptors. Small molecule drugs, A3AR-selective agonists, are currently in advanced clinical trials for the treatment of hepatocellular carcinoma, autoimmune inflammatory diseases, such as rheumatoid arthritis,...

Published: 7/25/2024 | Inventor(s): Kenneth Jacobson

Keywords(s): A3, ADENOSINE, ANTAGONISTS, BINDING, CA1CXX, CA1XXX, CAXXXX, CXXXXX, fluorescent, IA2XXX, IA3XXX, IAXXXX, IXXXXX, Molecular, Novel, Probes, RECEPTOR

Category(s): Collaboration Sought > Licensing, Application > Research Materials, Application > Diagnostics, TherapeuticArea > Dermatology, Application > Therapeutics, TherapeuticArea > Immunology, TherapeuticArea > Oncology

Triazole Derivatives of 4,7-disubstituted 2 naphthoic acid (PPTN) as P2Y14 Receptor Antagonists

The Molecular Recognition Section of NIDDK announces the availability of a novel triazole-based probes, structures which act as antagonists at human P2Y14 receptors. Although the physiologic functions of this receptor remain undefined, recently it has been strongly implicated in immune and inflammatory responses. Prior work with a 4,7-disubstituted...

Published: 7/25/2024 | Inventor(s): Evgeny Kiselev, Elisa Uliassi, Anna Junker, Kenneth Jacobson

Keywords(s): Alkyne, ANTAGONISTS, IB3XXX, IB4XXX, ID1XXX, P2Y14, Patent Category - Chemistry, Probe, RECEPTOR, small molecule, Structure-based, Triazole, VFXXXX, WIXXXX, WKXXXX, XHXXXX, YBXXXX

Category(s): Collaboration Sought > Collaboration, Application > Therapeutics, TherapeuticArea > Endocrinology, ResearchProducts > Research Equipment, TherapeuticArea > Immunology, TherapeuticArea > Pulmonology, Application > Research Materials

Truncated Methanocarba Adenosine Derivatives as A3 Adenosine Receptor Antagonists

Novel A3 adenosine antagonists available for licensing. A3 receptors are particularly highly expressed in inflammatory cells, making it a potentially desirable target for inflammatory diseases. This technology relates to highly specific antagonists and partial agonists of A3 adenosine receptors, which are negatively coupled to adenylate cyclase and...

Published: 9/3/2024 | Inventor(s): Kenneth Jacobson

Keywords(s): A3, ADENOSINE, ANTAGONISTS, Derivatives, IB3XXX, IBXXXX, IXXXXX, N-Methanocarba, Patent Category - Chemistry, RECEPTOR, TRUNCATED

Category(s): Collaboration Sought > Collaboration, Collaboration Sought > Licensing, Application > Research Materials, Application > Diagnostics, Application > Therapeutics, TherapeuticArea > Immunology

A Novel Treatment for Malarial Infections

The inventions described herein are antimalarial small molecule inhibitors of the plasmodial surface anion channel (PSAC), an essential nutrient acquisition ion channel expressed on human erythrocytes infected with malaria parasites. These inhibitors were discovered by high-throughput screening of chemical libraries and analysis of their ability to...

Published: 7/25/2024 | Inventor(s): Sanjay Desai

Keywords(s): Anion, ANTAGONISTS, ANTIMALARIAL, BBXXXX, BCXXXX, CHANNEL, DB2XXX, DBXXXX, Development, DRUG, DXXXXX, LEAD, Malaria, Malaria (Plasmodium sp.), MOLECULES, Plasmodial, Surface

Category(s): Collaboration Sought > Collaboration, Application > Therapeutics, TherapeuticArea > Infectious Disease

The Use of alpha-4 beta-7 integrin Inhibitors to Inhibit HIV Transmission and Infection

This invention involves the use of inhibitors of alpha-4 beta-7 (a4b7) integrin to inhibit HIV transmission/infection, as a prophylactic to inhibit onset of the acute stage of HIV infection or to treat HIV infection. The a4b7 integrin inhibitors were previously developed for use in other diseases, such as multiple sclerosis or inflammatory bowel disease. a4b7...

Published: 7/25/2024 | Inventor(s): Anthony Fauci, Claudia Cicala, Diana Goode, James Arthos

Keywords(s): ANTAGONISTS, BBXXXX, BETWEEN, DB4AXX, DB4XXX, DBXXXX, Direct, DXXXXX, gp120, HIV, INTERACTION, Intregrin, VLXXXX, YBXXXX, YCXXXX

Category(s): Collaboration Sought > Collaboration, Application > Therapeutics, TherapeuticArea > Infectious Disease

Vitamin D Receptor Antagonists for Treating Breast Cancer

Vitamin D receptor (VDR) is a nuclear receptor that is activated by calcitriol, the active form of vitamin D. It is best known for regulating dietary calcium uptake necessary for bone growth, but it also affects cell proliferation and differentiation. Therefore, it was thought that treatment with calcitriol or its derivatives could be useful to treat...

Published: 4/8/2024 | Inventor(s): Julianna Barsony

Keywords(s): ANTAGONISTS, ANTICANCER, CB7XXX, CBXXXX, CXXXXX, D, EFFECTS, Glioma, Novel, RECEPTOR, Vitamin

Category(s): Collaboration Sought > Licensing, Application > Therapeutics, TherapeuticArea > Oncology