Reuptake inhibitor
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Reuptake inhibitors (RIs) are a type of
psychostimulants.[1]
Most known reuptake inhibitors affect the
Mechanism of action
 | This section's factual accuracy is disputed. (January 2016) |
Active site transporter substrates
Standard reuptake inhibitors are believed to act simply as
extracellular concentrations of the neurotransmitter and therefore an increase in overall neurotransmission
.
Allosteric site transporter substrates
Alternatively, some reuptake inhibitors
allosteric sites and inhibit reuptake indirectly and noncompetitively
.
substrates such as cocaine and indatraline have lower affinity for these allosteric sites as well.[17][19][20]
A few of the
transporter protein and thereby modulating the affinity of substrates for the active site.[21] As a result, escitalopram has been marketed as an allosteric serotonin reuptake inhibitor. Notably, this allosteric site may be directly related to the above-mentioned PCP binding sites.[15][20]
Vesicular transporter substrates
A second type of reuptake inhibition affects
releasing agent. Pure vesicular reuptake inhibitors tend to actually lower synaptic neurotransmitter concentrations, as blocking the repackaging of, and storage of the neurotransmitter in question leaves them vulnerable to degradation via enzymes such as monoamine oxidase (MAO) that exist in the cytoplasm. With vesicular transport blocked, neurotransmitter
stores quickly become depleted.
irreversible inhibitor of the vesicular monoamine transporter 2
(VMAT2), and is a prototypical example of a vesicular reuptake inhibitor.
Indirect unknown mechanism
cation channel TRPC6.[24][27] Activation of TRPC6 induces the entry of calcium (Ca2+) and sodium (Na+) into the cell, which causes the effect through unknown mechanism.[27]
Types
Typical
- Amino acid reuptake inhibitor
- aspartatereuptake inhibitor)
- GABA reuptake inhibitor
- Glycine reuptake inhibitor
- Monoamine reuptake inhibitor
- Dopamine reuptake inhibitor
- Norepinephrine reuptake inhibitor
- Serotonin reuptake inhibitor
- Serotonin-norepinephrine reuptake inhibitor
- Norepinephrine-dopamine reuptake inhibitor
- Serotonin-dopamine reuptake inhibitor
- Serotonin-norepinephrine-dopamine reuptake inhibitor
- Miscellaneous
Atypical
- TRPC6 activators (wide-spectrum reuptake inhibitors) – hyperforin, adhyperforin
Plasmalemmal
- Choline reuptake inhibitor – hemicholinium-3, triethylcholine
Vesicular
- Vesicular acetylcholine transporter (VAChT) inhibitor – vesamicol
- Vesicular monoamine transporter (VMAT) inhibitor – reserpine, tetrabenazine
See also
- Releasing agent
References
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- ^ Barker, Eric L.; Randy D. Blakely (1995). Norepinephrine and serotonin transporters: molecular targets of antidepressant drugs. In: Psychopharmacology: the fourth generation of progress.
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- ^ PMID 7616423.
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- ^ PMID 9718074.
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- ^ S2CID 14097884.