Target intelligence / Profile preview

Solute carrier family 22 member 3 (OCT3)

Target
OCT3
Molecular classification
Transporter, Major facilitator superfamily (MFS), SLC22 family
01

Overview

Solute carrier family 22 member 3 (OCT3) is a plasma membrane polyspecific transporter belonging to the SLC22 family and the major facilitator superfamily (MFS)[1][5]. It mediates the electrogenic, sodium-independent transport of diverse endogenous (e.g., monoamines like dopamine and serotonin) and exogenous organic cations (drugs, toxins)[4][5]. OCT3 displays a broad tissue distribution, including heart, liver, kidney, placenta, brain, and other tissues[4][5][9]. Its function is critical for the low-affinity, high-capacity clearance of monoamines outside of neurons and for the disposition of therapeutic drugs and xenobiotics. OCT3 is targeted and inhibited by structurally diverse drugs and is modulated by stress hormones such as corticosterone[1][5]. Genetic variants and altered expression can influence susceptibility to metabolic, neuropsychiatric, and cardiovascular diseases, and underlie variability in drug response and toxicity[4][10]. Its wide substrate profile also means OCT3 plays a key role in drug-drug interactions in clinical pharmacology.

Other names
Organic cation transporter 3Extraneuronal monoamine transporter (EMT)SLC22A3
02

Mechanism of action

Inhibition or modulation of OCT3 alters the uptake and clearance of endogenous and exogenous organic cations, impacting levels of neurotransmitters, drug kinetics, and response to therapy[1][4][5][10].

03

Biological functions

Transport of organic cations (including catecholamines, monoamines, various drugs, xenobiotics)Regulation of neurotransmitter and hormone clearanceRenal clearance of cationic drugsRegulation of cardiac function and cellular metabolism
04

Disease associations

Neuropsychiatric diseaseCardiovascular diseaseMetabolic diseaseNeurodegenerative diseaseOther (implicated in various pathologies by altered transport function)
05

Safety considerations

Potential for drug-drug interactions due to broad substrate specificity[4][9].Changes in OCT3 function can alter pharmacokinetics and drug levels, impacting efficacy and toxicity[5].Inhibition by endogenous steroids (e.g., stress hormones) may alter neurotransmitter clearance, which could contribute to relapse in addiction or changes in mood regulation[5].
06

Interacting drugs

Decynium-22

9 more in the full profile.

07

Biomarkers

Genetic variants (polymorphisms) in SLC22A3/OCT3 may be associated with differences in metabolic rate, cardiovascular disease risk, and neuropsychiatric disorders[4].OCT3 expression can be a marker for predicting drug response (e.g., to metformin[10]).

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