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Allosteric serotonin reuptake inhibitor

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Allosteric serotonin reuptake inhibitor is a type of selective serotonin reuptake inhibitor (SSRI).

Escitalopram

Evidence of the allosteric action of escitalopram on the serotonin transported is based on the observation that the R isomer of citalopram can decrease the potency and inhibit the effects of the S isomer, probably through an allosteric interaction between two distinct, non-overlapping binding sites for the two different isomers on the serotonin transporter. Escitalopram, thus, binds not only to the primary site, but also to the allosteric site. From known SSRIs also paroxetine has action to the allosteric site, about half potency of escitalopram.

Vilazodone

Vilazodone has been shown to slow the disassociation rate of imipramine at the orthosteric of SERT by binding to a non-orthosteric pocket on the transporter.

References

  1. Mansari, Mostafa El; Wiborg, Ove; Mnie-Filali, Ouissame; Benturquia, Nadia; Sánchez, Connie; Haddjeri, Nasser (February 2007). "Allosteric modulation of the effect of escitalopram, paroxetine and fluoxetine: in-vitro and in-vivo studies". The International Journal of Neuropsychopharmacology. 10 (1): 31–40. doi:10.1017/S1461145705006462. ISSN 1461-1457. PMID 16448580.
  2. Plenge, Per; Yang, Dongxue; Salomon, Kristine; Laursen, Louise; Kalenderoglou, Iris E.; Newman, Amy H.; Gouaux, Eric; Coleman, Jonathan A.; Loland, Claus J. (2021-08-20). "The antidepressant drug vilazodone is an allosteric inhibitor of the serotonin transporter". Nature Communications. 12 (1): 5063. doi:10.1038/s41467-021-25363-3. ISSN 2041-1723. PMC 8379219.
Antidepressants (N06A)
Specific reuptake inhibitors and/or receptor modulators
SSRIsTooltip Selective serotonin reuptake inhibitors
SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors
NRIsTooltip Norepinephrine reuptake inhibitors
NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors
NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants
SARIsTooltip Serotonin antagonist and reuptake inhibitors
SMSTooltip Serotonin modulator and stimulators
Others
Tricyclic and tetracyclic antidepressants
TCAsTooltip Tricyclic antidepressants
TeCAsTooltip Tetracyclic antidepressants
Others
Monoamine oxidase inhibitors
Non-selective
MAOATooltip Monoamine oxidase A-selective
MAOBTooltip Monoamine oxidase B-selective
Adjunctive therapies
Miscellaneous
Serotonin receptor modulators
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT37
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7


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