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
Related Journals
Anti-Cancer Agents in Medicinal Chemistry
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry
Current Drug Safety
Current Drug Targets
Current Organic Chemistry
Current Organic Synthesis
Mini-Reviews in Organic Chemistry
Letters in Organic Chemistry
Letters in Drug Design & Discovery
Current Drug Discovery Technologies
Related Books
Advances in Organic Synthesis
Frontiers in Drug Design and Discovery
The Synthetic Methods, Structures, and Properties of the Ca-C σ Bond Organocalcium Containing Compounds
Advances in Organic Synthesis
Chemistry of Bipyrazoles: Synthesis and Applications
Frontiers in Cardiovascular Drug Discovery
Advances in Organic Synthesis
Advanced Nanocatalysis for Organic Synthesis and Electroanalysis
Frontiers in Drug Design and Discovery
Advances in Organic Synthesis
9