Abstract
The Vesicular Acetylcholine Transporter (VAChT) is found throughout the cholinergic nervous system and is responsible for transporting Acetylcholine (ACh) into synaptic vesicles for storage. Deterioration of cholinergic neurotransmission is a known pathophysiological hallmark of Alzheimers disease (AD). Ligands that bind to VAChT – particularly in the brain and CNS where cholinergic neurotransmission is vital for memory and cognitive function – may facilitate the study of cholinergic pathway regulation in the CNS and serve as useful diagnostic agents for AD. Vesamicol was the first VAChT ligand identified, however its poor selectivity has prompted the search for more potent and selective compounds. Numerous structural modifications to the vesamicol scaffold have been explored and several classes of VAChT ligands are highlighted in this review. The affinity and selectivity of these ligands for VAChT and -receptors are discussed.
Keywords: Alzheimer's disease, benzovesamicol, CNS, structure-activity relationship, VAChT, vesamicol
Current Bioactive Compounds
Title: Development of Vesicular Acetylcholine Transporter Ligands: Molecular Probes for Alzheimers Disease
Volume: 6 Issue: 3
Author(s): Nicolas Giboureau, Kylee M. Aumann, Corinne Beinat and Michael Kassiou
Affiliation:
Keywords: Alzheimer's disease, benzovesamicol, CNS, structure-activity relationship, VAChT, vesamicol
Abstract: The Vesicular Acetylcholine Transporter (VAChT) is found throughout the cholinergic nervous system and is responsible for transporting Acetylcholine (ACh) into synaptic vesicles for storage. Deterioration of cholinergic neurotransmission is a known pathophysiological hallmark of Alzheimers disease (AD). Ligands that bind to VAChT – particularly in the brain and CNS where cholinergic neurotransmission is vital for memory and cognitive function – may facilitate the study of cholinergic pathway regulation in the CNS and serve as useful diagnostic agents for AD. Vesamicol was the first VAChT ligand identified, however its poor selectivity has prompted the search for more potent and selective compounds. Numerous structural modifications to the vesamicol scaffold have been explored and several classes of VAChT ligands are highlighted in this review. The affinity and selectivity of these ligands for VAChT and -receptors are discussed.
Export Options
About this article
Cite this article as:
Giboureau Nicolas, M. Aumann Kylee, Beinat Corinne and Kassiou Michael, Development of Vesicular Acetylcholine Transporter Ligands: Molecular Probes for Alzheimers Disease, Current Bioactive Compounds 2010; 6 (3) . https://dx.doi.org/10.2174/157340710793237353
DOI https://dx.doi.org/10.2174/157340710793237353 |
Print ISSN 1573-4072 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6646 |
- 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
-
Hypertension in Older Patients
Current Hypertension Reviews Anti-Diabetic Compounds and their Patent Information: An Update
Recent Patents on Inflammation & Allergy Drug Discovery Nitric Oxide Related Therapeutic Phenomenon: A Challenging Task
Current Pharmaceutical Design The Pathophysiology of Heart Failure in Children: The Basics
Current Cardiology Reviews The Impact of Pharmacotherapy on the Cardiopulmonary Exercise Test Response in Patients with Heart Failure: A Mini Review
Current Vascular Pharmacology Adrenomedullin: Roles for Structure and Function in Cardiac or Vascular Tissues
Current Hypertension Reviews Drug-Related Cardiotoxicity for the Treatment of Haematological Malignancies in Elderly
Current Pharmaceutical Design MicroRNAs: Novel Diagnostic and Prognostic Biomarkers in Atherosclerosis
Current Topics in Medicinal Chemistry Active Metabolites Resulting from Decarboxylation, Reduction and Ester Hydrolysis of Parent Drugs
Current Drug Metabolism Targets for Anti-T. cruzi Drugs in the Post-Genomic Era
Current Enzyme Inhibition Potential Benefits of Glitazones for Cancer and Vascular Disease
Current Drug Therapy Recombinant Human Insulin-Like Growth Factor-1: A New Cardiovascular Disease Treatment Option?
Cardiovascular & Hematological Agents in Medicinal Chemistry Cardiovascular Effects of Green Tea Catechins: Progress and Promise
Recent Patents on Cardiovascular Drug Discovery Cardiac Nuclear Imaging: Current Status and Future Directions
Current Medical Imaging Immunophilins and Cardiovascular Complications
Current Medicinal Chemistry Nano-Delivery in Pediatric Tumors: Looking Back, Moving Forward
Anti-Cancer Agents in Medicinal Chemistry The Clinical Prognostic Value of LRG1 in Esophageal Squamous Cell Carcinoma
Current Cancer Drug Targets Influence of Ultrasound Mediated Transdermal Delivery of Losartan Potassium
Drug Delivery Letters Disparities in Cardiovascular Disease Risk in the United States
Current Cardiology Reviews Current Place of Beta-Blockers in the Treatment of Hypertension
Current Vascular Pharmacology