GPR 17 agonists and screening assay

Simple SummaryContent extracted from patent full text and abstract with AI.

This patent describes a new class of small molecule agonists for the GPR17 receptor—a G-protein coupled receptor implicated in various physiological and pathological processes. The invention also details screening assays that use these potent and selective agonists to identify modulators (especially antagonists) of GPR17, which could become candidate drugs for neurological, cardiovascular, and kidney diseases. The patent addresses the need for better agonists to enable effective high-throughput screening and drug discovery targeting GPR17.

Use CasesContent extracted from patent full text and abstract with AI.

• Development of pharmaceutical screening assays to discover new GPR17 antagonists or modulators.
• High-throughput drug screening for compounds to treat neurodegenerative diseases such as multiple sclerosis or stroke.
• Pharmacological research into GPR17 function and its role in signaling in the central nervous system, heart, and kidney.
• Identification and optimization of new drugs for the treatment or amelioration of ischemic diseases, neuropathic pain, and demyelinating disorders.
• Serving as robust chemical tools for studying GPR17 pharmacology in various biological and disease models.

BenefitsContent extracted from patent full text and abstract with AI.

• Provides highly potent and selective GPR17 agonists that work across different cell lines and systems, ensuring reliable screening conditions.
• Enables effective, reproducible, and cost-efficient high-throughput screening for GPR17 modulators, improving drug discovery pipelines.
• Facilitates the identification of promising therapeutic candidates for serious diseases like multiple sclerosis, stroke, cardiac and renal ischemia.
• Overcomes limitations of previously known GPR17 agonists, such as low potency, instability, and poor suitability for assays.
• Supports the development of new treatments for neuropathic pain and demyelinating diseases by providing both screening methods and candidate chemical entities.

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Patent Abstract

The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I.