Abstract
Significant progress in the development of potent and selective histamine H1-receptor agonists has been achieved since 1990. Optimisation of the class of 2-phenylhistamines has furnished 2-[3- (trifluoromethyl)phenyl]histamine and its Nα-methyl derivative. The discovery of histaprodifen (2-[2-(3,3- diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the novel lead compound suprahistaprodifen (Nα-2-[(1Himidazol- 4-yl)ethyl]histaprodifen) represents additional milestones in the H1-receptor agonist field.
Keywords: histaprodifen, suprahistaprodifen, h1-receptor agonist, partial agonist, guinea-pig ileum, guinea-pig aorta, guineapig trachea, rat aorta
Mini-Reviews in Medicinal Chemistry
Title: Structure-Activity Relationships of Histamine H1-Receptor Agonists
Volume: 4 Issue: 9
Author(s): Heinz H. Pertz, Sigurd Elz and Walter Schunack
Affiliation:
Keywords: histaprodifen, suprahistaprodifen, h1-receptor agonist, partial agonist, guinea-pig ileum, guinea-pig aorta, guineapig trachea, rat aorta
Abstract: Significant progress in the development of potent and selective histamine H1-receptor agonists has been achieved since 1990. Optimisation of the class of 2-phenylhistamines has furnished 2-[3- (trifluoromethyl)phenyl]histamine and its Nα-methyl derivative. The discovery of histaprodifen (2-[2-(3,3- diphenylpropyl)-1H-imidazol-4-yl]ethanamine) and the novel lead compound suprahistaprodifen (Nα-2-[(1Himidazol- 4-yl)ethyl]histaprodifen) represents additional milestones in the H1-receptor agonist field.
Export Options
About this article
Cite this article as:
Pertz H. Heinz, Elz Sigurd and Schunack Walter, Structure-Activity Relationships of Histamine H1-Receptor Agonists, Mini-Reviews in Medicinal Chemistry 2004; 4 (9) . https://dx.doi.org/10.2174/1389557043403198
DOI https://dx.doi.org/10.2174/1389557043403198 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
Call for Papers in Thematic Issues
Bioprospecting of Natural Products as Sources of New Multitarget Therapies
According to the Convention on Biological Diversity, bioprospecting is the exploration of biodiversity and indigenous knowledge to develop commercially valuable products for pharmaceutical and other applications. Bioprospecting involves searching for useful organic compounds in plants, fungi, marine organisms, and microorganisms. Natural products traditionally constituted the primary source of more than ...read more
Computational Frontiers in Medicinal Chemistry
The thematic issue "Computational Frontiers in Medicinal Chemistry" provides a robust platform for delving into state-of-the-art computational methodologies and technologies that significantly propel advancements in medicinal chemistry. This edition seeks to amalgamate top-tier reviews spotlighting the latest trends and breakthroughs in the fusion of computational approaches, including artificial intelligence (AI) ...read more
Natural Products and Dietary Supplements in Alleviation of Metabolic, Cardiovascular, and Neurological Disorders
Metabolic disorders like diabetes, obesity, inflammation, oxidative stress, cancer etc, cardiovascular disorders like angina, myocardial infarction, congestive heart failure etc as well as neurological disorders like Alzheimer?s, Parkinson?s, Epilepsy, Depression, etc are the global burden. They covered the major segment of the diseases and disorders from which the human community ...read more
Natural Products in Drug Discovery
Natural products have always been one of the important ways of drug discovery due to their novel skeleton and diverse functional group characteristics. According to statistics, between 1981 and 2019, the FDA approved a total of 1,394 small molecule drugs for marketing, of which 930 marketed drugs originated from the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Microbes, Immunity and Multiple Sclerosis: An Update
Current Immunology Reviews (Discontinued) Oral Inflammation and Bacteremia: Implications for Chronic and Acute Systemic Diseases Involving Major Organs
Cardiovascular & Hematological Disorders-Drug Targets Soft Matter Assemblies as Nanomedicine Platforms for Cancer Chemotherapy: A Journey from Market Products Towards Novel Approaches
Current Topics in Medicinal Chemistry Functions of Fukutin, a Gene Responsible for Fukuyama Type Congenital Muscular Dystrophy, in Neuromuscular System and Other Somatic Organs
Central Nervous System Agents in Medicinal Chemistry New Advances in Infant Feeding: New Products and Novel Technologies
Recent Patents on Food, Nutrition & Agriculture LC-MS for Simultaneous Determination of Vancomycin and Teicoplanin in Patient Plasma and its Application to Therapeutic Drug Monitoring
Current Pharmaceutical Analysis Combat Pneumococcal Infections: Adhesins as Candidates for Protein- Based Vaccine Development
Current Drug Targets Expression and Function of Cytokines and Chemokines in Neuropsychiatric Related Systemic Lupus Erythematosus
Current Rheumatology Reviews Autoimmune Neuromuscular Disorders
Current Neuropharmacology Prevalence of Asymptomatic Cryptococcal Antigenemia and Association with Follow-up Risk of Cryptococcal Meningitis and Mortality among HIV Infected Patients in North West India: A Prospective Cohort Study
Current HIV Research The CCL2/CCR2 Axis in the Pathogenesis of HIV-1 Infection: A New Cellular Target for Therapy?
Current Drug Targets Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas
Medicinal Chemistry Disease-Induced Neuroinflammation and Depression
CNS & Neurological Disorders - Drug Targets Antimicrobial Sulfated Glycans: Structure and Function
Current Topics in Medicinal Chemistry In Vivo Imaging of the Diseased Nervous System: An Update
Current Pharmaceutical Design Dysfunctions of the Diffusional Membrane Pathways Mediated Hemichannels in Inherited and Acquired Human Diseases
Current Vascular Pharmacology Immunomodulatory Properties of Antibiotics
Current Molecular Pharmacology Biologically Active Antimicrobial Compounds from Marine Microorganisms (2005-2019)
Current Pharmaceutical Biotechnology Brain Targeted Drug Delivery: Factors, Approaches and Patents
Recent Patents on Nanomedicine Cancer Metastasis: Characterization and Identification of the Behavior of Metastatic Tumor Cells and the Cell Adhesion Molecules, including Carbohydrates
Current Drug Targets - Cardiovascular & Hematological Disorders