Ajmalicine

Research use only, not for human use.

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 (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。(In Vitro):Ajmalicine preferentially blocks α1-adrenoceptor than α2-adrenoceptor. Ajmalicine inhibits contractions in a concentration-dependent manner, IC50=72.3 ± 22.5 μM. 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.(In Vivo):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.

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

Ajmalicine blocking 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. 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.

Raubasine | Delta-Yohimbine | Ajmalicin | Lamuran

Angiogenesis

Adrenergic Receptor

p53

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483-04-5

352.43

C21H24N2O3

>98% (HPLC)

In Vitro:?DMSO : 5.56 mg/mL (15.78 mM)

[H][C@@]12C[C@]3([H])C(=CO[C@@H](C)[C@@]3([H])CN1CCc1c2[nH]c2ccccc12)C(=O)OC

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(-20℃)

With Ice Pack

≥ 2 years