publication . Article . 2006

Therapeutic Potential of Monoamine Transporter Substrates

Richard B. Rothman; Michael H. Baumann;
Open Access
  • Published: 01 Sep 2006 Journal: Current Topics in Medicinal Chemistry, volume 6, pages 1,845-1,859 (issn: 1568-0266, Copyright policy)
  • Publisher: Bentham Science Publishers Ltd.
Abstract
Monoamine transporter proteins are targets for many psychoactive compounds, including therapeutic and abused stimulant drugs. This paper reviews recent work from our laboratory investigating the interaction of stimulants with transporters in brain tissue. We illustrate how determining the precise mechanism of stimulant drug action (uptake inhibitor vs. substrate) can provide unique opportunities for medication discovery. An important lesson learned from this work is that drugs which display equipotent substrate activity at dopamine (DA) and serotonin (5-HT) transporters have minimal abuse liability and few stimulant side-effects, yet are able to suppress ongoing...
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free text keywords: Drug Discovery, General Medicine, Fenfluramine, medicine.drug, medicine, business.industry, business, Monoamine transporter, biology.protein, biology, Substance abuse, medicine.disease, Serotonin, Stimulant, medicine.medical_treatment, Reuptake inhibitor, Dopamine, Amphetamine, Pharmacology
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