Allosteric serotonin reuptake inhibitor
Encyclopedia
Allosteric serotonin reuptake inhibitor is a marketing classification invented by the pharmaceutical company Lundbeck
for its selective serotonin reuptake inhibitor
(SSRI) escitalopram
, the S stereoisomer of the SSRI citalopram
. 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
.
The term allosteric refers to the negative interaction between the binding sites of to different drugs or isomers, however, it does not relate to the action of one drug to the inhibition of serotonin uptake. Allosteric serotonin reuptake inhibitors are therefore not a therapeutically distinct class of SSRI.
Lundbeck
H. Lundbeck A/S is a Danish international pharmaceutical company engaged in the research and development, production, marketing, and sale of drugs for the treatment of disorders in the central nervous system , including depression, schizophrenia, Alzheimer’s disease, Parkinson’s disease,...
for its selective serotonin reuptake inhibitor
Selective serotonin reuptake inhibitor
Selective serotonin re-uptake inhibitors or serotonin-specific reuptake inhibitor are a class of compounds typically used as antidepressants in the treatment of depression, anxiety disorders, and some personality disorders. The efficacy of SSRIs is disputed...
(SSRI) escitalopram
Escitalopram
Escitalopram is an antidepressant of the selective serotonin reuptake inhibitor class. It is approved by the U.S...
, the S stereoisomer of the SSRI citalopram
Citalopram
Citalopram brand names: Celexa, Cipramil) is an antidepressant drug of the selective serotonin reuptake inhibitor class. It has U.S...
. It is based on the observation that the R isomer of citalopram
Citalopram
Citalopram brand names: Celexa, Cipramil) is an antidepressant drug of the selective serotonin reuptake inhibitor class. It has U.S...
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
Serotonin transporter
The serotonin transporter is a monoamine transporter protein.This protein is an integral membrane protein that transports the neurotransmitter serotonin from synaptic spaces into presynaptic neurons. This transport of serotonin by the SERT protein terminates the action of serotonin and recycles it...
.
The term allosteric refers to the negative interaction between the binding sites of to different drugs or isomers, however, it does not relate to the action of one drug to the inhibition of serotonin uptake. Allosteric serotonin reuptake inhibitors are therefore not a therapeutically distinct class of SSRI.