An atypical antipsychotic and adrenergic

Iloperidone – 250 mg

Brand:
Cayman
CAS:
133454-47-4
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

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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SKU: 22957 - 250 mg Category:

Description

An atypical antipsychotic and adrenergic, dopamine, and serotonin receptor antagonist; binds to α1-AR, α2-AR, and D2 receptors (Kis = 0.31, 3, and 3.3 nM, respectively) as well as 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors (Kis = 33, 15, 0.2, and 14 nM, respectively) in human post-mortem brain tissue; binds to human D1, D3, D4, D5, and rat 5-HT2 receptors (Kis = 216, 7.1, 25, 319, and 3.1 nM, respectively); prevents the reduction in prepulse inhibition induced by apomorphine, PCP, and cirazoline in rats at 1-3 mg/kg; increases the time rats spend in the open arms of an elevated plus maze and the number of social interactions at 0.5 mg/kg, i.p.,

Formal name: 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]-ethanone

Synonyms: 

Molecular weight: 426.5

CAS: 133454-47-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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