m-Chlorophenylbiguanide hydrochloride 是一种 5-HT3 受体激动剂。它选择性结合 5-HT3(Ki: 0.002 μM) 超过 5-HT1A(Ki: 10 μM) 和 5-HT2(Ki: 10 μM) 受体,但也结合多巴胺转运蛋白上的高亲和力和低亲和力位点( DAT;IC50:在大鼠尾状壳核突触体膜中分别为 0.4 和 34.8 μM)。
产品描述
m-Chlorophenylbiguanide hydrochloride is a 5-HT3 receptor agonist. m-Chlorophenylbiguanide hydrochloride selectively binds 5-HT3(Ki: 0.002 μM) over 5-HT1A(Ki: 10 μM) and 5-HT2(Ki: 10 μM) receptors but also binds to high and low affinity sites on the dopamine transporter(DAT; IC50s: 0.4 and 34.8 μM, respectively, in rat caudate putamen synaptosomal membranes).
体内活性
m-Chlorophenylbiguanide hydrochloride induces depolarization of isolated rat vagus nerve and stimulates inositol phosphate formation in rat frontocingulate cortical slices (EC50s = 0.05 and 4.2 μM, respectively).m-Chlorophenylbiguanide hydrochloride induces bradycardia, an effect that can be reversed by the 5-HT3 receptor antagonist ondansetron, in anaesthetized cats (ED50 = 20.3 nmol/kg)[1].
Cas No.
2113-05-5
分子式
C8H11Cl2N5
分子量
248.11
别名
1-(3-氯苯基)双胍;1-(3-Chlorophenyl)biguanidehydrochloride
储存和溶解度
H2O:<20 mgml(80.61 mm)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years