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编 号:F358065
分子式:C21H25ClN2O3
分子量:388.89
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生物活性:
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity.

体内研究:
Ajmalicine hydrochloride blocking the pressor action of electrical stimulation and is active against sympathetic stimulation.Ajmalicine hydrochloride (0.5-4 mg/kg) induces a marked dose-dependent inhibition against the pressor response to noradrenaline.Animal Model:Male Wistar rats (300-350 g)
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.

体外研究:
Ajmalicine hydrochloride preferentially blocks α1-adrenoceptor than α2-adrenoceptor.Ajmalicine hydrochloride inhibits contractions in a concentration-dependent manner (IC50=72.3 ± 22.5 μM).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.
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