Илоперидон

Описание

Iloperidone is an atypical antipsychotic and adrenergic, dopamine, and serotonin (5-HT) receptor antagonist. It binds to several receptors, including the α₁-adrenergic receptor (α₁-AR), α₂-AR, and dopamine D₂ receptor (K_is = 0.31, 3, and 3.3 nM, respectively), as well as the 5-HT_1A, 5-HT_1D, 5-HT_2A, and 5-HT_2C receptors (K_is = 33, 15, 0.2, and 14 nM, respectively) in radioligand binding assays using human post-mortem brain tissue. Iloperidone also binds to human D₁, D₃, D₄, D₅, and rat 5-HT₂ receptors (K_is = 216, 7.1, 25, 319, and 3.1 nM, respectively, in CHO cells) and the histamine H₁ receptor (K_i = 12.3 nM in human post-mortem brain tissue). Iloperidone (1-3 mg/kg) prevents the reduction in prepulse inhibition induced by apomorphine , phencyclidine (PCP), and cirazoline in rats. 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. Formulations containing iloperidone have been used in the treatment of schizophrenia.

Химические свойства

Off-White Solid

Использование

Iloperidone (Fanapt, Fanapta, Zomaril) is an atypical antipsychotic for the treatment of schizophrenia. Iloperidone is a monoamine directed towards acting upon and antagonizing specific neurotransmitters, particularly multiple dopamine and serotonin recep

Определение

ChEBI: A member of the class of piperidines that is the 4-acetyl-2-methoxyphenyl ether of 3-(piperidin-1-yl)propan-1-ol which is substituted at position 4 of the piperidine ring by a 6-fluoro-1,2-benzoxazol-3-yl group. A member of the group of second generation a tipsychotics (also known as an atypical antipsychotics), it is used for the treatment of schizophrenia.

Общее описание

Iloperidone is an atypical antipsychotic administered for the treatment of schizophrenia. The drug is marketed under the trade names Fanapt and Fanapta. This Certified Spiking Solution^? is suitable for use in LC/MS or GC/MS applications including clinical toxicology, forensic testing, or pharmaceutical research.

Клиническое использование

Acting as an antagonist on serotonin (5-HT2) and dopamine receptor subtypes, iloperidone is an antipsychotic indicated for the treatment of acute schizophrenia in adults. Based on its in vitro and in vivo binding properties against both serotonin and dopamine receptors, it is expected that iloperidone will show fewer extrapyramidal symptoms than currently marketed antipsychotics such as haloperidol and clozapine. The original discovery was made by Hoechst-Roussel Pharmaceuticals who passed the developing rights to Vanda Pharmaceuticals and subsequently Novartis for marketing in the U.S. and Canada. While this drug was originally approved in the U.S. in 2009, the marketing was only initiated in the U.S. in 2010.