Abstract
Novel phenomena, such as constitutive activity and inverse agonism, have led to a ligand (re)classification along an agonists-neutral antagonist-inverse agonist continuum. This review focuses on adenosine A1 receptor ligands and their intrinsic activity (α). The intrinsic activity of a ligand depends both on the chemical characteristics of the compound itself and on the experimental conditions in which it is assayed. Consequently, due to this tissue-dependency determination of a ligands intrinsic activity is not always easily performed. Meanwhile, this feature may also be used in a profitable manner, namely to separate desired and unwanted effects of the drug. Briefly, this review provides possible screening methods to distinguish the different classes of ligands. It also deals with the structural elements and functional groups in the adenosine A1 receptor ligands that determine their intrinsic activity.
Keywords: adenosine receptor, inverse agonism, a1 receptor, intrinsic activity, partial agonism
Current Pharmaceutical Design
Title: Intrinsic Activity at Adenosine A1 Receptors: Partial and Inverse Agonism
Volume: 8 Issue: 26
Author(s): Rianne A.F. de Ligt and Ad P. Ijzerman
Affiliation:
Keywords: adenosine receptor, inverse agonism, a1 receptor, intrinsic activity, partial agonism
Abstract: Novel phenomena, such as constitutive activity and inverse agonism, have led to a ligand (re)classification along an agonists-neutral antagonist-inverse agonist continuum. This review focuses on adenosine A1 receptor ligands and their intrinsic activity (α). The intrinsic activity of a ligand depends both on the chemical characteristics of the compound itself and on the experimental conditions in which it is assayed. Consequently, due to this tissue-dependency determination of a ligands intrinsic activity is not always easily performed. Meanwhile, this feature may also be used in a profitable manner, namely to separate desired and unwanted effects of the drug. Briefly, this review provides possible screening methods to distinguish the different classes of ligands. It also deals with the structural elements and functional groups in the adenosine A1 receptor ligands that determine their intrinsic activity.
Export Options
About this article
Cite this article as:
de Ligt A.F. Rianne and Ijzerman Ad P., Intrinsic Activity at Adenosine A1 Receptors: Partial and Inverse Agonism, Current Pharmaceutical Design 2002; 8 (26) . https://dx.doi.org/10.2174/1381612023392874
DOI https://dx.doi.org/10.2174/1381612023392874 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...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
- Announcements
Related Articles
-
Meet Our Editorial Board Member
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) COX-2, Cell Proliferation and PMA in Head-and-Neck Cancer Cells
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) In Vivo Gastroprotective Effect of Nanoparticles: Influence of Chemical Composition and Volume Fraction
Current Pharmaceutical Design Haptoglobin Genotype Affects Inflammation after Aneurysmal Subarachnoid Hemorrhage
Current Neurovascular Research Role of Renin-Angiotensin System in Vascular Endothelial Dysfunction of Pregnancy-Induced Hypertension
Current Hypertension Reviews A Review of Clinical Studies Assessing the Therapeutic Efficacy of Escitalopram: A Step Towards Development
CNS & Neurological Disorders - Drug Targets Phosphoryl Chloride Mediated Synthesis of 5-Arylidene-2,4-Thiazolidinediones Derivatives via Aromatic Bisulfite Adducts
Letters in Organic Chemistry Biological Characteristics and Role of Histamine in Case of Allergic Rhinitis
Medicinal Chemistry Reviews - Online (Discontinued) Simultaneous multicolor luciferase reporter assays for monitoring of multiple genes expressions
Combinatorial Chemistry & High Throughput Screening Targeting Transient Receptor Potential Channels in Cardiometabolic Diseases and Myocardial Ischemia Reperfusion Injury
Current Drug Targets Pharmacological and Clinical Applications of Natriuretic Peptides: Accepted Knowledges or Changing Views?
Current Pharmaceutical Analysis Marine Peptides for Preventing Metabolic Syndrome
Current Protein & Peptide Science Minocycline and Doxycycline: More Than Antibiotics
Current Molecular Pharmacology Activated Immune System and Inflammation in Healthy Ageing: Relevance for Tryptophan and Neopterin Metabolism
Current Pharmaceutical Design Antioxidants in Health, Disease and Aging
CNS & Neurological Disorders - Drug Targets Studies on the IC50 of Metabolically Stable 1-(3,3-diphenylpropyl)- piperidinyl Amides and Ureas as Human CCR5 Receptor Antagonists Based on QSAR
Letters in Drug Design & Discovery Natural Radioprotective Agents: An Overview
Current Organic Chemistry Ovulation, Implantation and Placentation in Females with Obesity and Metabolic Disorders: Life in the Balance
Endocrine, Metabolic & Immune Disorders - Drug Targets Structure Activity Relationships of Novel Antiepileptic Drugs
Current Medicinal Chemistry Cell Penetrating Peptides for Tumor Targeting
Current Pharmaceutical Biotechnology