Ajmalicine 是一种有效的抗肾上腺素 (adrenolytic) 剂，优先阻断 α1-肾上腺素受体 (α1-adrenoceptor)。Ajmalicine 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂，IC50 为 72.3 μM。Ajmalicine 还可用于降压、蛇毒，具有镇静活性。

Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity。

Ajmalicine preferentially blocks α1-adrenoceptor than α2-adrenoceptor[1]. Ajmalicine inhibits contractions in a concentration-dependent manner, IC50=72.3 ± 22.5 μM[2]. Ajmalicine acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2[3].

Ajmalicine blocks the pressor action of electrical stimulation and is active against sympathetic stimulation. Ajmalicine (0.5-4 mg/kg) induces a marked dose-dependent inhibition against the pressor response to noradrenaline[1].

483-04-5

C21H24N2O3

352.43

阿吗里新;Ajmalicine

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years