ChemicalBook Product Catalog API Nervous system drugs Drug Metabolism in Human Brain AJMALICINE HYDROCHLORIDE

AJMALICINE HYDROCHLORIDE

Product NameAJMALICINE HYDROCHLORIDE
CAS4373-34-6
MFC21H25ClN2O3
MW388.89
EINECS224-471-9
MOL File4373-34-6.mol

Chemical Properties

Melting point

275-300 °C

Safety Information

Hazard Codes	Xn
Risk Statements	22-36/37/38
Safety Statements	26-36
WGK Germany	3
RTECS	AX7890000
F	10-23

MSDS

Provider	Language
SigmaAldrich	English

Usage And Synthesis

Uses

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].

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:	Male Wistar rats (300-350 g)^[1]
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.

IC 50

α1-adrenergic receptor; α2-adrenergic receptor

Purification Methods

This hydrochloride crystallises from MeOH or EtOH. Its solubility is 0.315g/100g of H2O at 100o. [Beilstein 27 III/IV 7928.]

References

[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. DOI:10.1016/0014-2999(84)90698-8
[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. DOI:10.1016/j.phymed.2009.10.008
[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 DOI:10.1111/j.1476-5381.1984.tb16514.x

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