2013Zhongguo yaolixue tongbaoRequires access

Research progress in monoamine transporters and monoamine transmitter reuptake inhibitors

You‐Zhi Zhang

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Abstract

Presynaptic membrane serotonin transporters(SERT) and norepinephrine transporter(NET),which are important neurotransmitter transporters,are responsible for reuptake of released serotonin(5-HT) and norepinephrine(NE),respectively.The major function of these transporters is to terminate monoamine transmission by mediating uptake of neurotransmitters from extracellular space into neurons and glial cells.Drugs that inhibit the activity of monoamine transporters produce increased neurotransmitter levels in the synaptic cleft,leading to their therapeutic use in depression.As SERT and NET are pharmacological targets for most antidepressants,understanding about the molecular pharmacology of these transporters,including their localization and function,molecular structure and regulation,as well as drug binding sites and mechanism of action,is important to new antidepressant development.

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What this paper is about

Presynaptic membrane serotonin transporters(SERT) and norepinephrine transporter(NET),which are important neurotransmitter transporters,are responsible for reuptake of released serotonin(5-HT) and norepinephrine(NE),respectively.The major function of these transporters is to terminate monoamine transmission by mediating uptake of neurotransmitters from extracellular space into neurons and glial cells.Drugs that inhibit the activity of monoamine transporters produce increased neurotransmitter levels in the synaptic cleft,leading to their therapeutic use in depression.As SERT and NET are pharmacological targets for most antidepressants,understanding about the molecular pharmacology of these transporters,including their localization and function,molecular structure and regulation,as well as drug binding sites and mechanism of action,is important to new antidepressant development.

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Available abstract

Presynaptic membrane serotonin transporters(SERT) and norepinephrine transporter(NET),which are important neurotransmitter transporters,are responsible for reuptake of released serotonin(5-HT) and norepinephrine(NE),respectively.The major function of these transporters is to terminate monoamine transmission by mediating uptake of neurotransmitters from extracellular space into neurons and glial cells.Drugs that inhibit the activity of monoamine transporters produce increased neurotransmitter levels in the synaptic cleft,leading to their therapeutic use in depression.As SERT and NET are pharmacological targets for most antidepressants,understanding about the molecular pharmacology of these transporters,including their localization and function,molecular structure and regulation,as well as drug binding sites and mechanism of action,is important to new antidepressant development.

Key concepts: Monoamine neurotransmitter, Reuptake, Norepinephrine transporter, Reuptake inhibitor, Antidepressant, Neurotransmitter, Neurotransmitter transporter, Synaptic cleft

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