Abstract
A series of gamma-amino alcohols were synthesized and screened for reuptake inhibition and noncompetitive NMDA antagonism. Compound (+/-)-3f simultaneously and potently inhibits reuptake of 5-HT, NE, and DA, representing a potential wide-spectrum reuptake inhibitor antidepressant. In addition, comparative rat and human studies uncovered a species-selective DA reuptake inhibitor (+/-)-2e, KD(hDAT)/KD(rDAT) = 97.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amino Alcohols / chemistry*
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Animals
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Antidepressive Agents / chemical synthesis*
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Antidepressive Agents / chemistry
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Antidepressive Agents / pharmacology
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Dopamine / metabolism*
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Humans
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Neurotransmitter Uptake Inhibitors / chemical synthesis*
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Neurotransmitter Uptake Inhibitors / chemistry
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Neurotransmitter Uptake Inhibitors / pharmacology
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Norepinephrine / metabolism*
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Rats
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Serotonin / metabolism*
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Species Specificity
Substances
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Amino Alcohols
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Antidepressive Agents
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Neurotransmitter Uptake Inhibitors
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Serotonin
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Dopamine
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Norepinephrine