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)
 
* <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.

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生物活性

製品説明 Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.
in vitro In CHO cells expressing human 5-HT1A receptors, perospirone shows a high affinity (Ki = 0.72 nM), and exhibits partial agonistic efficacy[1]. Perospirone changes epigenetic profiles of neural genes. It can cause DNA methylation changes in cell cultures[2]. 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[3].
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[1].

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.

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。

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