Product Introduction
Bioactivity


英文名: Itasetron

描述: Itasetron (U 98079A) 是一种5-羟色胺3受体拮抗剂，可用于预防大鼠与年龄有关的记忆缺陷。Itasetron 在癌症化疗和放疗动物模型中的止吐活性，可用于研究健忘症。

体内活性: Itasetron orally is rapidly absorbed (about 90 min), is highly bioavailable (greater than 90%), and has a long half-life (about 12 h). Itasetron (0.5, 1, 2, 4, and 8 mg; twice daily) in comparison with 8 mg b.i.d. ondansetron. Assessments were made in patients (n = 104) with histologically confirmed cancer (excluding head and neck tumors) and about to receive their first course of moderately emetogenic chemotherapy. Itasetron demonstrated comparable efficacy to ondansetron; no statistically significant between-group differences were observed in the primary (complete response rate) or secondary (nausea and delayed emesis) efficacy criteria. The tolerability of Itasetron was assessed as 'very good' or 'rather good' by 81% of patients and 89% of physicians. In conclusion, Itasetron is effective and well tolerated in patients receiving moderately emetogenic chemotherapy. Oral doses of 1 mg b.i.d. or above will be used in further clinical studies.[1]

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

溶解度: DMSO : 45 mg/mL (149.82 mM)


关键字: Itasetron

相关产品: Tropisetron hydrochloride | Perphenazine | Ramosetron | BRL 54443 | PF-03382792 | Tryptamine | Buspirone | Litoxetine | Dimebolin | Puerarin

相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library