AjmalicineAjmalicine
MedChemExpress (MCE)
HY-N1919
483-04-5
Raubasine
99.39%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 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 blocking the pressor action of electrical stimulation and is active against sympathetic stimulation[1]. Ajmalicine (0.5-4 mg/kg) induces a marked dose-dependent inhibition against the pressor response to noradrenaline[1].
α1-adrenergic receptor α2-adrenergic receptor
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[1]. Roquebert J, et al. Inhibition of the alpha 1 and alpha 2-adrenoceptor-mediated pressor response in pithed rats by raubasine, tetrahydroalstonine and akuammigine. Eur J Pharmacol. 1984 Oct 30
106(1):203-5. [Content Brief]
[2]. Pereira DM, et al. Pharmacological effects of Catharanthus roseus root alkaloids in acetylcholinesterase inhibition and cholinergic neurotransmission. Phytomedicine. 2010 Jul
17(8-9):646-52. [Content Brief]
[3]. Demichel P, et al. Effects of raubasine stereoisomers on pre- and postsynaptic alpha-adrenoceptors in the rat vas deferens. Br J Pharmacol. 1984 Oct
83(2):505-10 [Content Brief]