哌罗匹隆 T4576

Product Introduction
Bioactivity


英文名: Perospirone

描述: Perospirone (Lullan) 是具有口服活性的5-HT2A 受体和多巴胺 D2受体的拮抗剂，也是5-HT1A 受体的部分激动剂，Ki 分别为 0.6 、1.4和2.9 nM。它是一种非典型的抗精神病剂，可用于精神分裂症的研究。

细胞实验: 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.

动物实验: Animal Models: Five-week-old male ICR mice. Formulation: 0.5% methylcellulose solution. Dosages: 10 mg/kg, p.o.

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (128.94 mM)


关键字: 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

相关产品: Spiroxatrine | Zotepine | FGH31 | Pramipexole | Lurasidone hydrochloride | Hirsuteine | Fosopamine(HCl) | Mesoridazine Besylate | 3-CPMT | Fipexide

相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Parkinson's Disease Compound Library | Angiogenesis related Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Orally Active Compound Library

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