Histamine Receptors as Drug Targets

This book illustrates the current state-of-the-art in histamine research, with a focus on the appropriate methodologies to investigate the pharmacological properties and the therapeutic exploitation of HRs and their ligands. In addition, the range of techniques described provides an introduction to complementary cross-methodological disciplines beyond these fields. This multi-disciplinary approach is required to define the ‘decision gates’ that determine the development of more effective and safer therapeutic options for many forms of highly prevalent and debilitating diseases, such as asthma, dementias, dermatitis, and arthritis. Written for the Methods in Pharmacology and Toxicology series, chapters concentrate on practical, hands-on protocols from experts in the techniques.

1. Methodologies to Identify and Analyze Genetic Polymorphisms for Human Histamine Receptors

            Stephany Micallef and Astrid Sasse

 

2. Development, Characterization, and Validation of Anti-Human H₃ Receptor Isoform-Specific Antibodies

            Fiona C. Shenton, Natasha Lethbridge, and Paul L. Chazot

 

3. Approaches to Recombinant Histamine H₃/H₄ Receptor Expression in Mammalian Cells

            Tadeusz Karcz, Urszula Cichon, and Katarzyna Kiec-Kononowicz

 

4. Histamine H₂ Receptor Biased Signaling Methods

            Natalia Fernández, Carina Shayo, Carlos Davio, and Federico Monczor

 

5. Ligand-Binding Kinetics on Histamine Receptors

            Reggie Bosma, Tamara A.M. Mocking, Rob Leurs, and Henry F. Vischer

 

6. Methods to Study the Molecular Pharmacology of the Histamine H₄ Receptor

            Eléonore W.E. Verweij, Rob Leurs, and Henry F. Vischer

 

7. Chemiluminescence: A Sensitive Method for Detecting the Effects of Histamine Receptor Agonists/Antagonists on Neutrophil Oxidative Burst

            Ondrej Vašícek, Tomáš Perecko, Viera Jancinová, Silvia Pažoureková, Radomír Nosál, and Milan Cíž

 

8. Techniques Used in Pharmacological Evaluation of Histamine H₄ Receptor Function on Native Human Eosinophils

            Marek Grosicki and Katarzyna Kiec-Kononowicz

 

9. Assessment of the Efficacy of Histamine Receptor Antagonists in Murine Models of Atopic Dermatitis

            Kristine Roßbach, Hanna Köchling, Tomoki Fukuyama, Jenny Wilzopolski, Manfred Kietzmann, and Wolfgang Bäumer

 

10. Methodological Approaches to Study Histamine Pharmacology in the Kidney: From Cell Culture and Cell Imaging to Functional Assays and Electron Microscopy

            Alessandro Pini, Eleonora Veglia, Cristina Grange, and Arianna Carolina Rosa

 

11. Histamine and the Kidney: In Vivo Animal Models

            Alessandro Pini, Eleonora Veglia, and Arianna Carolina Rosa

 

12. Methodological Approaches to Investigate the Effects of Histamine Receptor Targeting Compounds in Preclinical Models of Breast Cancer

            Diego J. Martinel Lamas, Melisa B. Nicoud, Helena Sterle, Graciela P. Cricco, Gabriela A. Martin, Graciela A. Cremaschi, Hubert G. Schwelberger, Elena S. Rivera, and Vanina A Medina

 

13. Evaluation of Histidine Decarboxylase (HDC) Activity and Human Histamine Receptor 3 (H₃R) and HDC mRNA Levels

            Carlos Acosta-Andrade, José L Urdiales, Ignacio Fajardo, and Francisca Sánchez-Jiménez

 

14. Cerebrospinal Fluid Markers in Neuroinflammation: The Paradigm of Optic Neuritis

            Dimitrios P. Besinis and Maria C. Anagnostouli

 

15. In Vivo Diagnostic Procedures for IgE-Mediated Allergic Disorders

            Christopher Koulias, Xenophon Aggelides, Caterina Chliva, and Michael Makris

 

16. Dermatological Indications of Antihistamines

            Chrysovalantis Korfitis, Efstathios Rallis, and Dimitrios Rigopoulos

 

17. Histamine Quantification in Human Blood Samples

            Ekaterini Tiligada, Maria Kakolyri, and Madeleine Ennis