Perospirone NEW
Price | $37 | $61 | $113 |
Package | 5mg | 10mg | 25mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-16 |
Product Details
Product Name: Perospirone | CAS No.: 150915-41-6 |
Purity: 98.86% | Supply Ability: 10g |
Release date: 2024/11/16 |
Product Introduction
Bioactivity
名稱 | Perospirone |
描述 | Perospirone (Lullan) is an antagonist of serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist. |
細胞實驗 | Cell lines: Human neuroblastoma SK-N-SH cells. Concentrations: 10.5 or 105.5?nM.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. |
動物實驗 | Animal Models: Five-week-old male ICR mice. Formulation: 0.5% methylcellulose solution. Dosages: 10 mg/kg, p.o. |
體外活性 | 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]. |
體內(nèi)活性 | Perospirone shows potent 5-HT2 and D2 receptor blocking activities in various animal models in vivo. Perospirone inhibits various dopaminergic behaviours (e.g. methamphetamine-induced hyperactivity and apomorphine-induced stereotypy or climbing behaviour) in rodents. It also inhibits the rat conditioned avoidance response. In behavioural tests, perospirone markedly inhibits serotonergic behaviour (e.g. tryptamine-induced clonic seizures, and p-chlorphenamine-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 anaesthesia with ED50 values of 34 and 37 mg/kg (p.o.), respectively[1]. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 55 mg/mL (128.94 mM) |
關(guān)鍵字 | deficits | atypical | SM-9018 | Dopamine Receptor | 5-hydroxytryptamine Receptor | 5-HT Receptor | Orally | SM9018 | schizophrenic | disease | Serotonin Receptor | cognitive | Inhibitor | SM 9018 | inhibit | Perospirone | antipsychotic |
相關(guān)產(chǎn)品 | Alverine citrate | Dapoxetine hydrochloride | Octopamine hydrochloride | Oxolinic acid |
相關(guān)庫 | 經(jīng)典已知活性庫 | 疼痛相關(guān)化合物庫 | 神經(jīng)退行性疾病化合物庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 抗癌上市藥物庫 | 抗癌藥物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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