Ajmalicine hydrochloride  (Synonyms: Raubasine hydrochloride)

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

388.89

C₂₁H₂₅ClN₂O₃

4373-34-6

O=C(C1=CO[C@@H](C)[C@](CN2CC3)([H])[C@]1([H])C[C@@]2([H])C4=C3C5=CC=CC=C5N4)OC.[H]Cl

Room temperature in continental US; may vary elsewhere.

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

• [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]