利喷西平 T16758

Product Introduction
Bioactivity


英文名: Rispenzepine

描述: Rispenzepine 是一种新型的毒蕈碱型乙酰胆碱受体（mAChRs)的拮抗剂，选择性地靶向M1 和 M3 受体亚型，可用于治疗免疫系统疾病、感染、呼吸系统疾病。

体外活性: Rispenzepine almost fullly inhibits cholinergic, contractile responses at 0.3 μM (92.7±6.2% inhibition, n=6, p<0.05; pD2 value of 7.31±0.15). The M1, M1/M3, or M3 antagonists inhibit the EFS-evoked cholinergic contractile response in a concentration-dependent manner (4-DAMP > Rispenzepine > Pirenzepine), whereas Methoctramine facilitates this response at low concentrations (<3 μM). The presence of muscarinic autoreceptors in human and guinea pig trachea is investigated by comparing the effects of the muscarinic receptor antagonists Pirenzepine (M1), Methoctramine (M2), 4-DAMP (M3), and Rispenzepine (M1/M3) on cholinergic neural contractile responses evoked by electrical field stimulation (EFS) and [3H]ACh release. In ACh release studies, the M3 antagonist has no significant effect, whereas Pirenzepine, Methoctramine, and Rispenzepine significantly increase ACh release in guinea pig trachea [1].

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

关键字: Rispenzepine

利喷西平 T16758信息由TargetMol中国为您提供，如您想了解更多关于利喷西平 T16758报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途