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
