Perospirone hydrochloride

製品コードS4889 バッチS488901

印刷

化学情報

Chemical Structure Synonyms SM-9018 hydrochloride Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H30N4O2S.HCl
分子量 463.04 CAS No. 129273-38-7
Solubility (25°C)* 体外 DMSO 92 mg/mL (198.68 mM)
Water 5 mg/mL (10.79 mM)
 
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 Perospirone (SM-9018) は、セロトニン5HT2A受容体およびドーパミンD2受容体を拮抗する、アザピロンファミリーの非定型または第2世代抗精神病薬です。また、部分アゴニストとして5HT1A受容体にも親和性を示します。
in vitro In CHO cells expressing human 5-HT1A receptors, perospirone shows a high affinity (Ki = 0.72 nM), and exhibits partial agonistic efficacy. Perospirone changes epigenetic profiles of neural genes. It can cause DNA methylation changes in cell cultures. Perospirone is an inhibitor of Pgp which interferes directly and indirectly with the function of Pgp. The inhibition of Pgp by perospirone may cause clinically significant drug-drug interactions, especially in the tissue in which it accumulated.
in vivo Perospirone shows potent 5-HT2 and D2 receptor blocking activities in various animal models in vivo. Perospirone inhibits various dopaminergic behaviors (e.g. methamphetamine-induced hyperactivity and apomorphine-induced stereotypy or climbing behavior) in rodents. It also inhibits the rat conditioned avoidance response. In behavioral tests, perospirone markedly inhibits serotonergic behavior (e.g. tryptamine-induced clonic seizures, and p-chloramphetamine-induced hyperthermia) in rats. Perospirone has anxiolytic-like effects and mood stabilizing effects in various animal models. It inhibits motor coordination in a rota-rod test, and potentiates the duration of hexobarbital-induced anesthesia with ED50 values of 34 and 37 mg/kg (p.o.), respectively.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human neuroblastoma SK-N-SH cells
濃度 10.5 nM and 105.5 nM
反応時間 9 days
実験の流れ cells are maintained in Eagle's minimal essential medium containing 10% fetal bovine serum for 8 days. The cells are exposed to either a high dose (105.5 nM, assigned as the "high-dose group") or low dose (10.5 nM, assigned as the "low-dose group") of perospirone. The concentrations are determined based on dosages typically used in the clinical setting. The medium is changed on days 2, 5, and 8 with media containing perospirone, and on day 9, cells are harvested and processed.
動物実験 動物モデル Five-week old male ICR mice
投薬量 10 mg/kg
投与方法 p.o.

参考

  • http://booksandjournals.brillonline.com/content/journals/10.1163/1569391041501906
  • https://www.thieme-connect.com/DOI/DOI?10.1055/s-0044-101467
  • https://pubmed.ncbi.nlm.nih.gov/18478216/
  • https://pubmed.ncbi.nlm.nih.gov/16210777/

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：

NFX1-123: A potential therapeutic target in cervical cancer [ J Med Virol, 2023, 95(6):e28856] PubMed: 37288708

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。