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Targeting Serotonin (5-HT) Receptors for Developing Anti-Obesity Therapeutics

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Overview

Genome-wide association studies have confirmed the genetic link between 5-HT and obesity. It is found that 5-HT exerts its anorexic effects mainly through 5-HT 1B, 5-HT 2C, and 5-HT 6 receptors. These receptors may serve as primary targets for the treatment of obesity. Some potential anti-obesity drugs have been developed by targeting these receptors. In vivo and in vitro preclinical studies have found that these drugs worked by improving appetite and reducing body weight. Based on the profound research on obesity, Protheragen offers a customized 5-HT receptor-targeting anti-obesity therapeutic development service. Our goal is to accelerate the development of anti-obesity therapies targeting the 5-HT receptor through cutting-edge technology and comprehensive analyses and to provide extensive support for advancing our clients' research.

Excellent 5-HT Receptor-Targeting Anti-Obesity Therapy Development Service Rely on Professional Team

Each of our specialists has extensive expertise in all aspects of anti-obesity therapies and plays a key role in moving projects forward and delivering excellent outcomes. Specific services include the following:

Anti-Obesity Therapy Development

Anti-obesity drug development: Our anti-obesity drug development targets 5-HT receptor subtypes, including 5-HT 1B, 5-HT 2C, and 5-HT 6. Our goal is to develop anti-obesity drugs that are highly effective in areas such as appetite regulation and weight control without side effects.

  • Computer-aided Drug Design (CADD): We integrate computer simulation methods to explore anti-obesity drugs targeting 5-HT receptors. Our team facilitates the design and development of anti-obesity drugs by simulating and analyzing possible interactions between the 5-HT receptor and compounds of interest.
  • Research of anti-obesity drugs: We screen and synthesize selective 5-HT receptor agonists or antagonists. Then we evaluate the anti-obesity effects of these drugs through in vivo and in vitro experiments.
    • 5-HT 1B: Research into the mechanisms of obesity has identified the 5-HT 1B receptor as a potential target for the treatment of obesity. 5-HT 1B receptor knockout mice exhibit an increase in body weight and food intake compared to wild-type mice. After administration, we screen and synthesize 5-HT 1B receptor agonists and analyze the changes in appetite and body weight in animal models.
    • 5-HT 2C: 5-HT 2C receptor knockout mice overeat and eventually develop obesity. 5-HT 2C receptor agonists are an effective way to reduce body weight and control food intake. We evaluate the efficacy and safety of 5-HT 2C agonists to promote the development of anti-obesity drugs.
    • 5-HT 6: Assessment of the role of the 5-HT 6 receptor in obesity in rats and mice has identified this receptor as a potent target for the treatment of obesity. Selective 5-HT 6 receptor antagonists are found to reduce weight gain in animals and are a potential obesity treatment. We develop 5-HT 6 receptor antagonists and study their efficacy in obesity models.

Other therapies: In addition to this, we are happy to offer Gene Therapies targeting the 5-HT receptor, and combination therapy development services.

Preclinical Studies

We have extensive experience in preclinical studies of anti-obesity therapies, and meet the diverse testing requirements of our clients.

Obesity models: We construct a variety of obesity models to help evaluate the efficacy and safety of anti-obesity therapies targeting the 5-HT receptor. Animal models are widely recognized as a reliable option for analyzing the molecular mechanisms of obesity, evaluating preclinical studies of diet-induced obesity, and predicting anti-obesity therapies. Our animal models of obesity include various strains of small rodents (Mice, Rats), Rabbits, and others.

In vitro and in vivo studies: In vitro efficacy assessment is an important step in preclinical studies of anti-obesity therapies. We explore the binding affinity of anti-obesity drugs to 5-HT receptors and assess their in vitro toxicity. In addition to this, we have diet-induced models, mutation models, and Gene Editing Models. The safety, pharmacodynamics, and pharmacokinetics of anti-obesity therapies targeting the 5-HT receptor are evaluated by multiple routes and different modes of administration.

Workflow

No matter where you are in the development and pre-clinical study of anti-obesity therapies targeting the 5-HT receptor, we offer timely support.

Flowchart for the development of anti-obesity therapies targeting 5-HT. (Protheragen)

Applications

  • Understanding of the molecular mechanisms of obesity: Research on anti-obesity therapies targeting the 5-HT receptor is helping to advance a deeper understanding of the mechanisms of obesity.
  • Research on obesity-related complications: Obesity increases the risk of cardiovascular disease, diabetes, certain cancers, and others. The development of anti-obesity therapies targeting the 5-HT receptor is also critical to the study of therapies for these diseases.
  • Combination therapy: The use of two or more anti-obesity drugs with different mechanisms of action may be more effective. The development of anti-obesity drugs targeting the 5-HT receptor provides valuable clues to the study of combination therapies.

Advantages

  • One-stop process: We are committed to providing unrivaled research services, and assisting you from initial consultation, anti-obesity therapy development, and pre-clinical studies to data interpretation.
  • Strict project standards: We have a set of strict project standards to ensure the consistency and accuracy of experimental data.
  • Best after-sales service: We also provide strong after-sales support. Our professional scientific support team is always ready to answer and solve any questions.

What Other Services Do We Offer for Obesity Research?

Our team brings together researchers from diverse backgrounds to provide innovative solutions and support obesity research and the development of anti-obesity therapies. We not only understand the risk of obesity through comprehensive genetic and environmental analyses but also utilize advanced diagnostic tests and obesity prediction to provide data to support the development of obesity intervention strategies. Obesity biomarkers and microbiome analysis play an important role in obesity research. We also provide comprehensive biomarker and microbiome analysis services and translate the data into sound insights. We also specialize in various obesity-related gene editing techniques and use them to study the effectiveness of gene editing in therapy. Our team is also responsible for developing specialized weight loss and weight management programs to help achieve scientific weight management and obesity interventions.

Publication

Technology: Molecular modeling, Thin layer chromatography

Journal: Molecules

IF: 3.06

Published: 2018

Results: In the present study, the affinity and in vivo anti-obesity activity of several novel synthetic aromatic triazine-methylpiperazines towards 5-HT receptors were evaluated by computer-assisted conformational relationship analysis, in vivo and in vitro studies. The results showed that one of the compounds exhibited the highest anti-obesity and antidepressant activity without in vitro cytotoxicity. This study provides data support for the design, synthesis, and preclinical studies of anti-obesity drugs.

Fig.1 Development process for 5-HT receptor ligands.Fig.1 Detailed flow of the entire analysis. (Kurczab, et al., 2018)

Frequently Asked Questions

What is the role of CADD in anti-obesity drug development?

CADD is based on theoretical computational methods of molecular structure and uses computer simulations to predict the interaction between anti-obesity drugs and their targets. It provides valuable information for designing and optimizing drug molecules by predicting whether binding is possible and its binding strength. We provide molecular dynamics simulation and molecular docking services to support the development of anti-obesity drugs.

  • Molecular dynamics simulation uses equations of motion to calculate the velocity and temporal position of system atoms during interactions to generate clues about interactions and molecular motion.
  • Molecular docking is used to predict binding patterns between anti-obesity drug candidates and specific biological targets and provide information about binding conformation and binding affinity.

Apart from 5-HT receptors, what other targets are used in studies related to the treatment of obesity?

The molecular mechanisms of obesity are complex and influenced by multiple factors. With the deepening of obesity research, more and more targets are being discovered and used to develop anti-obesity therapies, such as Melanocortin 4 Receptor, Peroxisome Proliferator-Activated Receptors, Cannabinoid Receptors, and so on. In addition to the 5-HT Receptor, we also provide anti-obesity therapeutic development services targeting these receptors.

At Protheragen, our research team brings together highly skilled experts with diverse backgrounds for the research and development of anti-obesity therapies targeting the 5-HT receptor. Welcome to contact us if you have any needs or doubts in this area.

Reference

  1. Kurczab, R.; et al. Computer-aided studies for novel arylhydantoin 1, 3, 5-triazine derivatives as 5-HT6 serotonin receptor ligands with antidepressive-like, anxiolytic and antiobesity action in vivo. Molecules. 2018, 23(10): 2529.

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.

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