Abstract
The dopamine transporter (DAT) is a target for the development of pharmacotherapies for a number of central disorders including Parkinsons disease, Alzheimers disease, schizophrenia, Tourettes syndrome, Lesch-Nyhan disease, attention deficit hyperactivity disorder (ADHD), obesity, depression, and stimulant abuse as well as normal aging. Considerable effort continues to be devoted to the development of new ligands for the DAT. In this review, we present some of the more interesting ligands developed during the last few years from the 3-phenytropane, 1,4-dialkylpiperazine, phenylpiperidine, and benztropine classes of DAT uptake inhibitors as well as a few less studied miscellaneous DAT uptake inhibitors. Studies related to the therapeutic potential of some of the more studied compounds are presented. A few of the compounds have been studied as pharmacotherapies for Parkinsons disease, ADHD, and obesity. However, most of the drug discovery studies have been directed toward pharmacotherapies for stimulant abuse (mainly cocaine). A number of the compounds showed decreased cocaine maintained responding in rhesus monkeys trained to self-administer cocaine. One compound, GBR 12,909, was evaluated in a Phase 1 clinical trial.
Keywords: Dopamine transporter, 3-phenyltropane, 1,4-dialkylpiperazine, phenylpiperidine, benztropine
Current Topics in Medicinal Chemistry
Title: Dopamine Transporter Ligands: Recent Developments and Therapeutic Potential
Volume: 6 Issue: 17
Author(s): Scott P. Runyon and F. Ivy Carroll
Affiliation:
Keywords: Dopamine transporter, 3-phenyltropane, 1,4-dialkylpiperazine, phenylpiperidine, benztropine
Abstract: The dopamine transporter (DAT) is a target for the development of pharmacotherapies for a number of central disorders including Parkinsons disease, Alzheimers disease, schizophrenia, Tourettes syndrome, Lesch-Nyhan disease, attention deficit hyperactivity disorder (ADHD), obesity, depression, and stimulant abuse as well as normal aging. Considerable effort continues to be devoted to the development of new ligands for the DAT. In this review, we present some of the more interesting ligands developed during the last few years from the 3-phenytropane, 1,4-dialkylpiperazine, phenylpiperidine, and benztropine classes of DAT uptake inhibitors as well as a few less studied miscellaneous DAT uptake inhibitors. Studies related to the therapeutic potential of some of the more studied compounds are presented. A few of the compounds have been studied as pharmacotherapies for Parkinsons disease, ADHD, and obesity. However, most of the drug discovery studies have been directed toward pharmacotherapies for stimulant abuse (mainly cocaine). A number of the compounds showed decreased cocaine maintained responding in rhesus monkeys trained to self-administer cocaine. One compound, GBR 12,909, was evaluated in a Phase 1 clinical trial.
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Cite this article as:
Runyon P. Scott and Carroll F. Ivy, Dopamine Transporter Ligands: Recent Developments and Therapeutic Potential, Current Topics in Medicinal Chemistry 2006; 6 (17) . https://dx.doi.org/10.2174/156802606778249775
DOI https://dx.doi.org/10.2174/156802606778249775 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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