Ace Therapeutics provides a wide range of specialized services for the development of 5-HT receptor antagonists, offering comprehensive support to advance the discovery and optimization of these therapeutics. We have extensive experience in the design and synthesis of molecules targeting 5-HT receptor subtypes. Our in vitro and in vivo pharmacology platforms allow comprehensive characterization of receptor binding affinities, mechanism of action, efficacy, and safety profiles of your drug candidates.
The Role of 5-HT Receptors in GI and Liver Diseases
5-HT receptors, also known as serotonin receptors, are a diverse family of receptors found throughout the body, playing crucial roles in mood, cognition, and gastrointestinal function. In the digestive system, 5-HT receptors regulate intestinal secretion, bile flow, and hepatic blood flow. Dysregulation of these receptors has been implicated in conditions such as irritable bowel syndrome (IBS), functional dyspepsia, and non-alcoholic fatty liver disease (NAFLD). Their widespread involvement in gastrointestinal and liver diseases makes 5-HT receptors promising targets for therapeutic interventions.
Figure 1. How 5-HT signaling contributes to liver fibrosis. (Redenšek Trampuž S., et al., 2024)
What Can We Do for the Development of 5-HT Receptor Antagonists?
- Target Validation & Profiling
Using cell lines and animal models, we support researchers in their exploration of specific 5-HT receptor subtypes in the pathogenesis of gastrointestinal and liver diseases. We utilize techniques such as siRNA knockdown, CRISPR-Cas9 gene editing, and overexpression studies to manipulate the expression of specific 5-HT receptor subtypes and assess their effect on disease progression.
- Discovery and Optimization of 5-HT Receptor Antagonists
| Items |
Service Introduction |
| In Silico Screening |
We offer advanced molecular modeling and in silico screening to identify and design potential lead compounds that can effectively target 5-HT receptors. |
| High-Throughput Screening (HTS) |
Our high-throughput screening (HTS) services enable rapid screening of large compound libraries to identify those with strong binding affinities to 5-HT receptors. |
| Lead Optimization |
Our medicinal chemistry team specializes in optimizing lead compounds to enhance their efficacy, selectivity, and safety profiles. Our services involve structure-activity relationship (SAR) studies, compound synthesis, and iterative testing and refinement. |
Preclinical Evaluation Services for 5-HT Receptor Antagonists
In Vitro Evaluation
In Vivo Evaluation
- Target Selectivity: We utilize a range of techniques to assess the binding affinity, potency, and selectivity of 5-HT receptor antagonists for specific 5-HT receptor subtypes, including radioligand binding assays, calcium flux assays and cAMP accumulation assays.
- 3D Spheroid Models: We can develop 3D gastrointestinal and liver spheroid models that mimic the complex microenvironment of tissues, to evaluate the efficacy and selectivity of 5-HT receptor antagonists in a more physiologically relevant setting.
We conduct preclinical studies in relevant animal models of gastrointestinal and liver diseases to help you assess the efficacy of 5-HT receptor antagonists in reducing disease severity.
With our deep understanding of 5-HT receptors and their role in various gastrointestinal and liver diseases, Ace Therapeutics is committed to delivering high-quality services that accelerate the development of effective 5-HT receptor antagonists. Contact us today to discuss how our expertise can contribute to your 5-HT antagonist development program.
References
- Redenšek Trampuž S., et al. Mechanisms of 5-HT receptor antagonists in the regulation of fibrosis in a 3D human liver spheroid model. Sci Rep. 2024, 14(1):1396.
- Kato S. Role of serotonin 5-HT3 receptors in intestinal inflammation. Biol Pharm Bull. 2013, 36(9):1406-9.
Related Services
Our products and services are for research use only and can not be used for diagnostic or other purposes.
