Definition
ChEBI: A maleate salt obtained by reaction of paroxetine with one equivalent of maleic acid. Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (Ki = 0.05 nM). Ki values are 1.1, 350 and 1100 nM for inhibi
ion of [3H]-5-HT, [3H]-l-NA and [3H]-DA uptake respectively. Displays minimal affinity for alpha1-, alpha2- or beta-adrenoceptors, 5-HT2A, 5-HT1A, D2
General Description
Paroxetine, marketed under trade names such as Paxil? or Aropax, is an SSRI antidepressant used to treat many conditions in adults from major depression and obsessive-compulsive disorder to several anxiety disorders. Suitable uses for this certified solution standard include as a starting material for calibrators and controls in LC/MS or GC/MS paroxetine testing applications such as urine drug testing, prescription monitoring, clinical toxicology, or forensic analysis.
Biological Activity
Highly potent and selective 5-HT uptake inhibitor that binds with high affinity to the serotonin transporter (K i = 0.05 nM). K i values are 1.1, 350 and 1100 nM for inhibition of [ 3 H]-5-HT, [ 3 H]-l-NA and [ 3 H]-DA uptake respectively. Displays minimal affinity for a 1 -, a 2 - or b-adrenoceptors, 5-HT 2A , 5-HT 1A , D 2 or H 1 receptors at concentrations below 1000 nM, however displays weak affinity for muscarinic ACh receptors (K i = 42 nM). Antidepressant and anxiolytic in vivo .
Biochem/physiol Actions
Paroxetine is a strong cytochrome P450 2D6 isotype (CYP2D6) inhibitor, which reduces the effectiveness of tamoxifen. This phenylpiperidine derivative inhibits clozapine metabolism. Paroxetine is used to treat social phobia, obsessive-compulsive disorder and panic disorder. It is also used to treat the premenstrual dysphoric disorder, post-traumatic stress disorder and chronic headache.
