Abstract
The first antagonists known for the histamine H3 receptor were mono-substituted imidazolecontaining compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.
Keywords: cipralisant, ciproxifan, clobenpropit, h3 receptor, imidazole, sch 79687, radioligand, thioperamide
Mini-Reviews in Medicinal Chemistry
Title: Medicinal Chemical and Pharmacological Aspects of Imidazole-Containing Histamine H3 Receptor Antagonists
Volume: 4 Issue: 9
Author(s): Holger Stark, Markus Kathmann, Eberhard Schlicker, Walter Schunack, Birgit Schlegel and Wolfgang Sippl
Affiliation:
Keywords: cipralisant, ciproxifan, clobenpropit, h3 receptor, imidazole, sch 79687, radioligand, thioperamide
Abstract: The first antagonists known for the histamine H3 receptor were mono-substituted imidazolecontaining compounds like thioperamide. Meanwhile numerous novel leads have been developed possessing improved affinities, selectivities, specificities, and pharmacokinetic properties. Scope and limitations of this promising class are discussed concerning their structure-activity relationships as well as pharmacological and potential therapeutic aspects.
Export Options
About this article
Cite this article as:
Stark Holger, Kathmann Markus, Schlicker Eberhard, Schunack Walter, Schlegel Birgit and Sippl Wolfgang, Medicinal Chemical and Pharmacological Aspects of Imidazole-Containing Histamine H3 Receptor Antagonists, Mini-Reviews in Medicinal Chemistry 2004; 4 (9) . https://dx.doi.org/10.2174/1389557043403107
DOI https://dx.doi.org/10.2174/1389557043403107 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |

- Author Guidelines
- Bentham Author Support Services (BASS)
- 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
- Announcements
Related Articles
-
Drug-induced Inhibition and Trafficking Disruption of ion Channels: Pathogenesis of QT Abnormalities and Drug-induced Fatal Arrhythmias
Current Cardiology Reviews Recombinant Hepatitis B Vaccination in Renal Failure Patients
Current Pharmaceutical Biotechnology Antineoplastic Activity of Monocrotaline Against Hepatocellular Carcinoma
Anti-Cancer Agents in Medicinal Chemistry Multi-target Drug Discovery via PTML Modeling: Applications to the Design of Virtual Dual Inhibitors of CDK4 and HER2
Current Topics in Medicinal Chemistry Hypertension, Diabetes and Neurodegenerative Diseases: Is there a Clinical Link through the Ca2+/cAMP Signalling Interaction?
Current Hypertension Reviews Vascular Protection to Increase the Safety of Tissue Plasminogen Activator for Stroke
Current Pharmaceutical Design Microglial Activation and its Implications in the Brain Diseases
Current Medicinal Chemistry A Review of the Relationships among the Key Determinants Affecting the Mental Health Disorders of the People in Greater Mekong Subregion Countries
Current Psychiatry Reviews Family Psychoeducation in Clinical High Risk and First-Episode Psychosis
Adolescent Psychiatry Multiparametric MRI Evaluation of Developmental Venous Anomalies in the Brain: Association with Signal Changes on FLAIR in Patients with Multiple Sclerosis
Current Medical Imaging Silymarin Extends Lifespan and Reduces Proteotoxicity in C. elegans Alzheimer’s Model
CNS & Neurological Disorders - Drug Targets Editorial (Thematic Issue: Emerging Targets for Stimulant Use Disorders: Where To Invest In An Era Of Constrained Resources?)
CNS & Neurological Disorders - Drug Targets Modulation of Eating by Central Catecholamine Systems
Current Drug Targets Elucidation of the Chromatographic Enantiomer Elution Order Through Computational Studies
Mini-Reviews in Medicinal Chemistry Glutathione-Related Factors and Oxidative Stress in Autism, A Review
Current Medicinal Chemistry The Effectiveness of Topical Cannabidiol Oil in Symptomatic Relief of Peripheral Neuropathy of the Lower Extremities
Current Pharmaceutical Biotechnology 1,4-Dihydropyridines as Tools for Mitochondrial Medicine Against Oxidative Stress and Associated Metabolic Disorders
Current Organic Chemistry The Current Use of Mass Spectrometry in Combination with Other Separation Techniques in Drug Discovery Arena
Medicinal Chemistry Modeling and Simulation Studies of Human β3 Adrenergic Receptor and its Interactions with Agonists
Current Computer-Aided Drug Design Inhibitors of Nitrogen Oxide Species Production in Animal Models of Inflammation and Future Directions for Therapy in Inflammatory Disorders
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents