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A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
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Histamine H3 receptor antagonists/inverse agonists: Where do they go?
Nakisa Ghamari1, Omid Zarei2, José-Antonio Arias-Montaño3
1Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran; School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Pharmacology & Therapeutics
|April 28, 2019
Summary
Histamine H3 receptor antagonists show promise for treating CNS, metabolic, and allergic diseases. However, clinical development faces significant challenges and requires further investigation.
Area of Science:
- Pharmacology
- Neuroscience
- Drug Development
Background:
- The histamine H3 receptor, discovered in 1983, is a key target in various physiological processes.
- Significant preclinical advancements have been made in developing H3 receptor antagonists/inverse agonists.
Purpose of the Study:
- To review the role of H3 receptors in central nervous system, metabolic, and allergic diseases.
- To assess the current status of H3 receptor antagonists/inverse agonists in clinical trials.
- To highlight the challenges in developing these drug candidates.
Main Methods:
- Literature review of preclinical and clinical studies.
- Analysis of the pathophysiology of H3 receptor-related diseases.
- Evaluation of clinical trial data and developmental hurdles.
Main Results:
- H3 receptor antagonists/inverse agonists have demonstrated therapeutic potential in preclinical models.
- Several drug candidates have progressed to clinical trials for diverse indications.
- Developmental pathways are hindered by various challenges impacting market entry.
Conclusions:
- H3 receptor antagonists/inverse agonists represent a promising therapeutic avenue.
- Overcoming developmental obstacles is crucial for successful drug commercialization.
- Further research is needed to fully realize the clinical potential of H3 receptor modulators.
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