Formulation: A solid
Formal Name: 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-(methoxy-d3)phenyl]-ethanone
Purity: ≥99% (deuterated forms d1-d3)
Formula Markup: C24H24D3FN2O4
Formula Weight: 429,5
Shelf life (days): 1460
CAS Number: 1071167-49-1
Notes: Iloperidone-d3 is intended for use as an internal standard for the quantification of iloperidone (Item No. 22957) by GC- or LC-MS. Iloperidone is an atypical antipsychotic and adrenergic, dopamine, and serotonin (5-HT) receptor antagonist.{39863} It binds to several receptors, including the α1-adrenergic receptor (α1-AR), α2-AR, and dopamine D2 receptor (Kis = 0.31, 3, and 3.3 nM, respectively), as well as the 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors (Kis = 33, 15, 0.2, and 14 nM, respectively) in radioligand binding assays using human post-mortem brain tissue.{25511} Iloperidone also binds to human D1, D3, D4, D5, and rat 5-HT2 receptors (Kis = 216, 7.1, 25, 319, and 3.1 nM, respectively, in CHO cells) and the histamine H1 receptor (Ki = 12.3 nM in human post-mortem brain tissue).{39864,25511} Iloperidone (1-3 mg/kg) prevents the reduction in prepulse inhibition induced by apomorphine (Item No. 16094), phencyclidine (PCP), and cirazoline (Item No. 21791) in rats.{39863} It also increases the time rats spend in the open arms of the elevated plus maze and the number of social interactions when administered at a dose of 0.5 mg/kg.{39865} Formulations containing iloperidone have been used in the treatment of schizophrenia.
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