Iloperidone

製品コードS1483 バッチS148301

印刷

化学情報

Chemical Structure Synonyms HP873 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H27FN2O4
分子量 426.48 CAS No. 133454-47-4
Solubility (25°C)* 体外 DMSO 27 mg/mL (63.3 mM)
Ethanol 4 mg/mL (9.37 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Iloperidone（HP873）は、統合失調症の治療に使用されるドーパミン（D2）/セロトニン（5-HT2）受容体拮抗薬です。
in vitro Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors. This compound displays higher affinity for the dopamine D3 receptor (Ki = 7.1 nM) than for the dopamine D4 receptor (Ki = 25 nM). It displays high affinity for the 5-HT6 and 5-HT7 receptors (Ki = 42.7 nM and 21.6 nM, respectively), and is found to have higher affinity for the 5-HT2A (Ki = 5.6 nM) than for the 5-HT2C receptor (Ki = 42.8 nM). This chemical significantly increases dopa accumulation, an index of dopamine turnover in response to D2 receptor blockade, at doses from 0.3 mg/kg to 10 mg/kg i.p. in the striatum and from 1 mg/kg to 10 mg/kg in the nucleus accumbens.
in vivo Iloperidone exerts behavioral effects in pharmacological rats models of disrupted sensorimotor gating consistent with "atypical" antipsychotics, mediated by antagonism of dopaminergic and noradrenergic receptors. This compound (1 and 3 mg/kg) prevents the PPI-disruptive effects of treatment with 1 mg/kg PCP. It (0.3 mg/kg) prevents cirazoline-induced PPI deficits, independent of its effects on startle magnitude. This chemical (10 mg/kg) and Melperone (10 mg/kg) produce an equivalent or a smaller increase in DA release in the nucleus accumbens (NAC) of rats, respectively, compared to the mPFC, whereas none of them increase acetylcholine (ACh) release in the NAC.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/11750183/
  • https://pubmed.ncbi.nlm.nih.gov/8997630/
  • https://pubmed.ncbi.nlm.nih.gov/8768747/
  • https://pubmed.ncbi.nlm.nih.gov/16762376/
  • https://pubmed.ncbi.nlm.nih.gov/12445705/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A Low Dose of Aripiprazole Has the Strongest Sensitization Effect Among 19 Repositioned Bipolar Drugs in P-gp-overexpressing Drug-resistant Cancer Cells [ Anticancer Res, 2021, 41(2):687-697] PubMed: 33517273
Exploring the kinetic selectivity of antipsychotics for dopamine D2 and 5-HT2A [ bioRxiv, 2021, 10.1101/2021.11.14.468520] PubMed: None
Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. [ Sci Rep, 2018, 8(1):15753] PubMed: 30361678

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。