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Ajmalicine hydrochloride

CAS: 4373-34-6 F: C21H25ClN2O3 W: 388.89

Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalic
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Bioactivity 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[1][2].
Invitro Ajmalicine hydrochloride preferentially blocks α1-adrenoceptor than 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].
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:
Name Ajmalicine hydrochloride
CAS 4373-34-6
Formula C21H25ClN2O3
Molar Mass 388.89
Transport Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Reference [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. [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. [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