Synthesis of (1S,2R)-1-Phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide (PPDC) Derivatives Modified at the Carbamoyl Moiety As a New Class of NMDA Receptor Antagonists

Kazuta, Yuji; Tsujita, Ryuichi; Ogawa, Kiyoshi; Hokonohara, Tadami; Yamashita, Kanako; Morino, Kiyoko; Matsuda, Akira; Shuto, Satoshi

doi:10.1016/s0968-0896(02)00030-5

Cited by 13 publications

(3 citation statements)

References 21 publications

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“…These compounds exhibited antidepressant-like characteristics equal to imipramine in well-accepted rat models of antidepressant effect; both PRC025 and PRC050 increased time spent swimming and reduced time spent immobile in the forced swim test and reduced time spent immobile in the tail suspension test [39]. Several milnacipran derivatives have been developed in search of molecules with more potent N-methyl-D-aspartic acid (NMDA) antagonism [23,42 cited in 37]. More recently, analogs have been synthesized to evaluate their relative monoamine transporter inhibition potency and selectivity.…”

Section: Examples Of Compounds In Developmentmentioning

confidence: 99%

Triple Reuptake Inhibitors: The Next Generation of Antidepressants

Marks¹,

Pae²,

Patkar³

2008

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Depression has been associated with impaired neurotransmission of serotonergic, norepinephrinergic, and dopaminergic pathways, although most pharmacologic treatment strategies for depression enhance only serotonin and norepinephrine neurotransmission. Current drug development efforts are aimed at a new class of antidepressants which inhibit the reuptake of all three neurotransmitters in the hope of creating medications with broader efficacy and/or quicker onset of action. The current review explores limitations of presently available antidepressants and the history and premise behind the movement to devise triple reuptake inhibitors. The evidence for and against the claim that broader spectrum agents are more efficacious is discussed. Examples of triple reuptake inhibitors in development are compared, and preclinical and clinical research with these agents to date is described.

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Section: Examples Of Compounds In Developmentmentioning

confidence: 99%

Triple Reuptake Inhibitors: The Next Generation of Antidepressants

Marks¹,

Pae²,

Patkar³

2008

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“…Milnacipran has been also recognized as non-competitive NMDA receptor antagonist [51,52]. Although the binding affinity of milnacipran for the NMDA receptor is not very high, the compounds have the advantage of sufficiently penetrating into the brain without serious side effects [21,52,53] as described above.…”

Section: Discussionmentioning

confidence: 99%

Effects of Milnacipran in Animal Models of Anxiety and Memory

et al. 2006

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Serotonin (5-HT) and noradrenaline (NA) are involved in both pathogenesis and recovery from depression and anxiety. We examined the effects of acute and chronic treatment with milnacipran, a serotonin/noradrenaline reuptake inhibitors (SNRIs) antidepressant, on anxiety and memory retention in rats. Male Wistar rats received acute or chronic administration of milnacipran (12.5, 25 or 50 mg/kg) or saline (control group). The animals were separately submitted to elevated plus-maze, inhibitory avoidance and open-field tasks 1 h after injection, in the acute group, or 23 h after last injection, in the chronic group. Our results showed an anxiolytic-like effect after chronic administration of milnacipran at doses of 25 and 50 mg/kg. The treatment does not interfere in memory retention and habituation to a novel environment at any doses studied. These findings support that milnacipran, an established SNRIs antidepressant, can also be useful in the treatment of anxiety disorders.

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“…Two families of compounds in development are analogs of the dual reuptake inhibitors milnacipran and venlafaxine. Several milnacipran derivatives have been developed in search of molecules with more potent N-methyl-D-aspartic acid (NMDA) antagonism 42,43. More recently, analogs have been synthesized to evaluate their relative monoamine transporter inhibition potency and selectivity.…”

Section: Compounds In Developmentmentioning

confidence: 99%

Triple Reuptake Inhibitors: A Premise and Promise

Marks

Pae

Patkar

2008

Psychiatry Investig

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On the horizon there is a new class of psychoactive medications which work by inhibiting the neuronal reuptake of serotonin, norepinephrine, and dopamine. There are multiple potential indications for these drugs. Research suggests that they may have a role in treating depressive disorders, and it is plausible they may have potential efficacy in obesity, addiction, and pain syndromes. The current review describes some of the molecules in development presently and explores the research relevant to possible clinical uses for this class of medications.

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Synthesis of (1S,2R)-1-Phenyl-2-[(S)-1-aminopropyl]-N,N-diethylcyclopropanecarboxamide (PPDC) Derivatives Modified at the Carbamoyl Moiety As a New Class of NMDA Receptor Antagonists

Cited by 13 publications

References 21 publications

Triple Reuptake Inhibitors: The Next Generation of Antidepressants

Triple Reuptake Inhibitors: The Next Generation of Antidepressants

Effects of Milnacipran in Animal Models of Anxiety and Memory

Triple Reuptake Inhibitors: A Premise and Promise

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