Ajmalicine (Raubasine) hydrochloride 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 hydrochloride 是一种可逆性但非竞争性尼古丁受体 (nicotine receptor) 完全抑制剂,其IC50为 72.3 μM。Ajmalicine hydrochloride 还可用于降压、蛇毒,具有镇静活性。
生物活性 | Ajmalicine (Raubasine) hydrochloride is a potentadrenolyticagent which preferentially blocksα1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitivenicotine receptorfull inhibitor, with anIC50of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity[1][2]. |
IC50& Target | α1-adrenergic receptor | α2-adrenergic receptor |
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体外研究 (In Vitro) | Ajmalicine hydrochloride preferentially blocksα1-adrenoceptorthan α2-adrenoceptor[1]. Ajmalicine hydrochloride inhibits contractions in a concentration-dependent manner (IC50=72.3 ± 22.5 μM)[2]. Ajmalicine hydrochloride 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].
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体内研究 (In Vivo) | Ajmalicine hydrochloride blocking the pressor action of electrical stimulation and is active against sympathetic stimulation[1]. Ajmalicine hydrochloride (0.5-4 mg/kg) induces a marked dose-dependent inhibition against the pressor response to noradrenaline[1].
Animal Model: | Male Wistar rats (300-350 g)[1] | Dosage: | 0.5, 1, 2, and 4 mg/kg | Administration: | IV, once | Result: | Induced a marked dose-dependent inhibition against the pressor response to noradrenaline. |
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来源 | - Plants
- Rosaceae
- Rosa multifoloraThunb
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |