5-ht2b Selective Inhibitors
ID U-4922
Category Therapeutics
Subcategory Small Molecule
Researchers
Brief Summary
A novel family of 5HT2B-selective antagonists for neuropathologies and other conditions.
Problem Statement
Serotonin receptors are popular targets for many diseases, particularly neuropathologies. The existence of 14 subtypes, however, necessitates selective ligands. Current drugs tend to bind non-selectively to 5-HT2A and 5-HT2C as well as 5-HT2B, limiting their use.
Technology Description
The proposed antagonists offer increased selectivity to 5-HT2B. These compounds exhibit nanomolar to micromolar selective interactions, which increases efficacy and reduces side effects of therapeutics. 5HT2B has additional potential applications in gastrointestinal, cardiac, and bone marrow related conditions.
Stage of Development
Optimization & Testing
Benefit
- Increased specificity.
- Improved binding affinity.
- Represents a new chemical class with various applications.
Publications
Lin Z, Smith M, Concepcion G, Haygood M, Olivera B, Light A, Schmidt E. (2017). Modulating the serotonin receptor spectrum of pulicatin natural products. Journal of Natural Products. 80(8): 2360-2370. doi: 10.1021/acs.jnatprod.7b00317.
IP
Publication Number: US-2014-0018400-A1
Patent Title: Methods and Compositions Related to Neuroactive Thiazoline Compounds
Jurisdiction/Country: United States
Application Type: Non-Provisional
Contact Info
Jason Young
(801) 587-0519
jason.r.young@utah.edu
