title: Triple reuptake inhibitors: a patent review (2006 - 2012).
abstract: BACKGROUND
  The dysfunctions of three very important monoamine neurotransmitters, serotonin (5-HT), norepinephrine (NE) and dopamine (DA), are associated with some of important CNS diseases such as depression; developing the triple reuptake inhibitors (TRIs) that can rebalance 5-HT, NE and DA through the inhibition of the monoamine reuptake transporters will lead to a more effective and safer antidepressant.
  
  
  METHODS
  This article reviews past 7 years' advances in the development of TRIs; a patent review (2006 - 2012), covering the discovery of new chemical entities, and development status of leading TRI clinical candidates.
  
  
  CONCLUSIONS
  The development of TRIs has several challenges, including discovering a "single" agent that has the activities against all three monoamine reuptake transporters SERT, NET and DAT. More important is that the agent must have a "right ratio" to be safer and better tolerated for the treatment of depression. The TRIs can potentially be used for the treatment of other CNS diseases, such as pain, Parkinson's and attention deficit hyperactivity disorder (ADHD), depending on ratios of SERT, NET and DAT.
authors.affiliation: Fudan University, School of Pharmacy, Department of Medicinal Chemistry , 826 Zhangheng Road, Pudong Xinqu, Shanghai, 201203 , P.R. China +86 21 51980126 ; limingshao@fudan.edu.cn.
authors.forename: Liming
authors.initials: L
authors.lastname: Shao
authors.forename: Wei
authors.initials: W
authors.lastname: Li
authors.forename: Qiong
authors.initials: Q
authors.lastname: Xie
authors.forename: Hong
authors.initials: H
authors.lastname: Yin
mesh_terms: D018759:Adrenergic Uptake Inhibitors / Q000494:pharmacology; D000818:Animals; D000928:Antidepressive Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D018765:Dopamine Uptake Inhibitors / Q000494:pharmacology; D015195:Drug Design; D004335:Drug and Narcotic Control; D006801:Humans; D015394:Molecular Structure; D014179:Neurotransmitter Uptake Inhibitors / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D010330:Patents as Topic; D017367:Selective Serotonin Reuptake Inhibitors / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D018759:Adrenergic Uptake Inhibitors; D000928:Antidepressive Agents; D018765:Dopamine Uptake Inhibitors; D014179:Neurotransmitter Uptake Inhibitors; D017367:Selective Serotonin Reuptake Inhibitors