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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
5-HT2C receptor modulators: a patent survey
Junwon Lee1, Myung Eun Jung, Jinhwa Lee
1Green Cross Corporation, Research Center, Giheung-Gu, Yongin, Gyeonggi-Do, 446-770, Republic of Korea.
Expert Opinion on Therapeutic Patents
|September 21, 2010
Summary
Selective 5-HT(2C) receptor modulators show promise for treating CNS disorders. Ongoing research focuses on identifying compounds with proven clinical efficacy and safety for conditions like obesity and schizophrenia.
Area of Science:
- Pharmacology and Medicinal Chemistry
- Central Nervous System (CNS) Disorders
- G Protein-Coupled Receptors (GPCRs)
Background:
- The serotonin 5-HT(2C) receptor, a GPCR, is a key target in the CNS for psychiatric medications.
- Dysregulation of 5-HT(2C) receptor activity is linked to numerous unmet medical needs, including obesity, schizophrenia, depression, and addiction.
- Developing potent and selective 5-HT(2C) receptor modulators is of significant therapeutic interest.
Purpose of the Study:
- To review research progress on 5-HT(2C) receptor modulators reported in patent literature from 2003-2010.
- To provide a medicinal chemist's perspective on structure-activity relationships for 5-HT(2C) modulators.
- To identify key pharmaceutical companies involved in 5-HT(2C) receptor modulator development.
Main Methods:
- Comprehensive review of patent literature published between January 2003 and June 2010.
- Focus on identifying novel chemical structures and their interactions with the 5-HT(2C) receptor.
- Analysis of patent filings to track industry-driven research and development efforts.
Main Results:
- Overview of diverse 5-HT(2C) receptor modulators identified in patents over an 8-year period.
- Characterization of structural classes demonstrating interaction with the 5-HT(2C) receptor.
- Identification of leading pharmaceutical companies and their contributions to the field.
Conclusions:
- Substantial evidence supports the therapeutic potential of selective 5-HT(2C) receptor modulators for CNS disorders.
- Several promising modulators with high functional selectivity have been identified, but clinical data are still limited.
- The search for 5-HT(2C) receptor modulators with proven clinical efficacy and safety remains an active area of research.
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