ILOPERIDONE Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Iloperidone is an atypical antipsychotic and adrenergic, dopamine, and serotonin (5-HT) receptor antagonist. It binds to several receptors, including the α
1-adrenergic receptor (α
1-AR), α
2-AR, and dopamine D
2 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 D
1, D
3, D
4, D
5, and rat 5-HT
2 receptors (K
is = 216, 7.1, 25, 319, and 3.1 nM, respectively, in CHO cells) and the histamine H
1 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.
Chemische Eigenschaften
Off-White Solid
Verwenden
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
Definition
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.
Allgemeine Beschreibung
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.
Clinical Use
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.
ILOPERIDONE Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
