Trifluoperazine-d3 (hydrochloride)

Trifluoperazine-d3 is intended for use as an internal standard for the quantification of trifluoperazine (Item No. 15068) by GC- or LC-MS. Trifluoperazine (TFP) is a phenothiazine compound with anti-adrenergic and anti-dopaminergic actions typical of antipsychotic agents.{24253} It antagonizes adrenergic receptors, with selectivity for a1 over the a2 subtypes (Kis = 24, 653, 163, and 391 nM for a1A, a2A, a2B, and a2C, respectively). TFP binds with much higher affinity to the dopamine D2-like receptor (Kd = 0.96 nM) compared to the dopamine D4-like and the serotonin 5-HT2A receptors (Kds = 44 and 135 nM, respectively).{24252} Furthermore, TFP antagonizes calmodulin (CaM) and alters the calcium-binding properties of calsequestrin (CSQ).{23719,24254} TFP has been shown to activate type-2 ryanodine receptors independently of its CaM and CSQ activity.{24254}