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AJMALICINE HYDROCHLORIDE

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AJMALICINE HYDROCHLORIDE Basic information

Product Name:
AJMALICINE HYDROCHLORIDE
Synonyms:
  • RAUBASINE HYDROCHLORIDE
  • ajmalicine,monohydrochloride
  • gamma-yohimbinehydrochloride
  • gamma-yohimbinhydrochloride
  • oxayohimban-16-carboxylicacid,16,17-didehydro-19-methyl-,methylester,mon
  • D-YOHIMBINE
  • DELTA-YOHIMBINE HYDROCHLORIDE
  • AJMALICINE HCL
CAS:
4373-34-6
MF:
C21H25ClN2O3
MW:
388.89
EINECS:
224-471-9
Mol File:
4373-34-6.mol
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AJMALICINE HYDROCHLORIDE Chemical Properties

Melting point:
275-300 °C
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Safety Information

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

MSDS

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AJMALICINE HYDROCHLORIDE 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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