Ace Therapeutics is dedicated to supporting the development of innovative H2 Receptor Blockers for gastrointestinal diseases, such as peptic ulcers, gastroesophageal reflux disease (GERD), and Zollinger-Ellison syndrome. We offer a comprehensive suite of services that encompass the entire preclinical drug development pipeline, including screening and optimization of H2 receptor blockers and preclinical testing to evaluate their efficacy and safety.
The Role of H2 Receptors in Gastrointestinal Diseases
H2 receptors on stomach parietal cells regulate gastric acid secretion by triggering the release of hydrochloric acid (HCl) when they bind to histamine. While essential for digestion, overproduction of gastric acid can cause mucosal damage, inflammation, and ulceration, leading to diseases such as peptic ulcers, GERD, and Zollinger-Ellison syndrome. H2 receptor blockers block the action of histamine, effectively reducing gastric acid secretion, healing ulcers, and alleviating acid-related symptoms, highlighting their potential as key treatments for gastrointestinal diseases.
Figure 1. Molecular mechanisms and receptors involved in regulating acid secretion from parietal cells. (Yadav S., et al., 2024)
What Can We Do for the Development of H2 Receptor Blockers?
- Medicinal Chemistry Services
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| Lead Identification and Optimization |
Utilize high-throughput screening, virtual screening, and structure-based drug design to identify and optimize novel H2 receptor blocker candidates with improved potency, selectivity, and pharmacokinetic properties. |
| Analog Synthesis and Structure-Activity Relationship (SAR) Studies |
Synthesize and evaluate a series of analogs to understand the structure-activity relationship of H2 receptor blockers in order to determine optimal chemical structures for ideal efficacy and safety. |
- In Vitro Pharmacology Services
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| Binding Assays |
Perform in vitro binding assays to determine the affinity and selectivity of H2 receptor blockers for the H2 receptor compared to other histamine receptors (H1, H3, and H4). |
| Functional Assays |
Utilize cell-based assays to evaluate the functional activity of H2 receptor blockers in inhibiting histamine-stimulated gastric acid secretion in isolated gastric cells or cell lines. |
| Selectivity Studies |
Assess the selectivity of H2 receptor blockers against other targets relevant to gastrointestinal function, such as muscarinic receptors, serotonin receptors, and other GPCRs. |
- In Vivo Pharmacology Services
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| Custom Animal Models |
We utilize animal models of gastrointestinal diseases, such as peptic ulcer disease, GERD, and Zollinger-Ellison syndrome, to evaluate the efficacy of your H2 receptor blockers in reducing gastric acid secretion, promoting ulcer healing, and alleviating disease symptoms. |
| Pharmacodynamic Studies |
We assess the pharmacodynamic effects of your H2 receptor blockers in vivo, including changes in gastric pH, gastric emptying rate, and other relevant disease parameters. |
| Pharmacokinetic Studies |
We conduct pharmacokinetic studies in animals to determine the absorption, distribution, metabolism, and excretion of your H2 receptor blockers, informing optimal dosing regimens and formulation strategies. |
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| Safety Assessment |
We can conduct acute and chronic toxicity studies in multiple animal species to evaluate the safety and tolerability of H2 receptor blockers. |
| Studies of Off-target Effects |
We investigate potential off-target effects and toxicological effects to evaluate the potential adverse effects of your H2 receptor blockers on the cardiovascular, respiratory, and central nervous systems. |
Ace Therapeutics offers comprehensive solutions for H2 receptor blocker development in the field of gastrointestinal and liver diseases. We provide customized services in drug design, disease modeling, and preclinical studies. If you are looking for a collaborative partner to help move your H2 blocker towards the clinical research, please contact us.
References
- Yadav S., et al. From lab to nature: Recent advancements in the journey of gastroprotective agents from medicinal chemistry to phytotherapy. Eur J Med Chem. 2024, 272:116436.
- Nugent C.C. et al. H2 blockers. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing. 2024.
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