Target intelligence / Profile preview

Serotonin and Norepinephrine Transporters (SERT and NET)

Target
SERT and NET
Molecular classification
Transporters, Membrane transport proteins, Sodium-dependent neurotransmitter transporters, Monoamine transporters
01

Overview

The serotonin transporter (SERT) and norepinephrine transporter (NET) are sodium-dependent neurotransmitter transporters responsible for the reuptake of released serotonin and norepinephrine, respectively, into nerve terminals in the brain. These transporters play key roles in spatiotemporal regulation of neurotransmission, maintenance of extrasynaptic monoamine levels, and pre-synaptic monoamine homeostasis. They are important targets for antidepressant medications, particularly serotonin-norepinephrine reuptake inhibitors (SNRIs), which block the reuptake of both serotonin and norepinephrine, thereby increasing their availability in the synaptic cleft. This dual inhibition can offer advantages over single-neurotransmitter targeting drugs by addressing a wider range of symptoms, especially in conditions involving both mood disorders and pain.

Other names
Serotonin Transporter (SERT)Norepinephrine Transporter (NET)Noradrenaline Transporter (NAT)Solute carrier family 6 member 2 (SLC6A2) for NET
02

Mechanism of action

Inhibition of serotonin and norepinephrine reuptake from synaptic cleft, blocking reabsorption of neurotransmitters, and increasing availability of serotonin and norepinephrine in the brain.

03

Biological functions

Neurotransmitter reuptakeRegulation of neurotransmitter concentrations in synaptic cleftMaintenance of extrasynaptic monoamine levelsPre-synaptic monoamine homeostasisRegulation of moodRegulation of pain signaling
04

Disease associations

DepressionAnxiety disordersChronic neuropathic painFibromyalgiaAttention-deficit hyperactivity disorder (ADHD)Obsessive-compulsive disorder (OCD)Menopausal symptoms
05

Safety considerations

Increased risk of suicidal thoughts or behavior in children, teens, and adults under 25Serotonin syndrome (potentially life-threatening)Withdrawal symptomsSexual dysfunctionNausea, dry mouth, dizziness, headache, insomniaIncreased sweatingConstipation
06

Interacting drugs

Venlafaxine

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