Norepinephrine transporter inhibitors and their therapeutic potential.
Article Details
- CitationCopy to clipboard
Zhou J
Norepinephrine transporter inhibitors and their therapeutic potential.
Drugs Future. 2004 Dec;29(12):1235-1244.
- PubMed ID
- 16871320 [ View in PubMed]
- Abstract
The norepinephrine transporter (NET) is located in the plasma membrane of noradrenergic neurons, where it functions to take up synaptically released norepinephrine (NE). The NET thus serves as the primary mechanism for the inactivation of noradrenergic signaling. Some potent and selective or mixed NET inhibitors (e.g., reboxetine and atomoxetine) have been successfully developed to treat a variety of mental disorders such as depression and attention deficit hyperactivity disorder (ADHD). However, to date, only a very limited number of NET-selective inhibitors are available. New potent and selective NET inhibitors may find application in the treatment of mental disorders or in PET imaging, and may enhance our basic understanding of these illnesses. In the present review, both previously reported and newly designed NET inhibitors, as well as their therapeutic and imaging potential, will be discussed. Two types of molecules, the conformationally constrained tropanes and the piperidine-based nocaine/modafinil hybrid ligands, represent new leads and provide good opportunities for discovering novel potent and selective NET inhibitors that are useful as therapies and imaging agents for the NET.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Nisoxetine Sodium-dependent serotonin transporter Protein Humans UnknownNot Available Details - Drug Transporters
Drug Transporter Kind Organism Pharmacological Action Actions Nortriptyline Sodium-dependent noradrenaline transporter Protein Humans UnknownSubstrateInhibitorDetails