Allosteric serotonin reuptake inhibitor
Allosteric serotonin reuptake inhibitor is a type of selective serotonin reuptake inhibitor (SSRI). Currently only escitalopram, the S stereoisomer of the SSRI citalopram is included in this category. It 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.[1]
References
- 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.
- Connie Sánchez (2006). "The Pharmacology of Citalopram Enantiomers: The Antagonism by R-Citalopram on the Effect of S-Citalopram". Basic & Clinical Pharmacology & Toxicology. 99 (2): 91–5. doi:10.1111/j.1742-7843.2006.pto_295.x. PMID 16918708.
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