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Ajmalicine

Catalog No. T8044   CAS 483-04-5
Synonyms: Lamuran, Delta-Yohimbine, Raubasine, Ajmalicin

Ajmalicine (Raubasine) (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity。

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Ajmalicine Chemical Structure
Ajmalicine, CAS 483-04-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 113.00
2 mg In stock $ 168.00
5 mg In stock $ 283.00
10 mg In stock $ 422.00
25 mg In stock $ 688.00
50 mg In stock $ 957.00
100 mg In stock $ 1,290.00
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Purity: 96.9%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ajmalicine (Raubasine) (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, IC50 = 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity。
In vitro Ajmalicine preferentially blocks α1-adrenoceptor than α2-adrenoceptor[1]. Ajmalicine inhibits contractions in a concentration-dependent manner, IC50=72.3 ± 22.5 μM[2]. Ajmalicine 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 blocks the pressor action of electrical stimulation and is active against sympathetic stimulation. Ajmalicine (0.5-4 mg/kg) induces a marked dose-dependent inhibition against the pressor response to noradrenaline[1].
Synonyms Lamuran, Delta-Yohimbine, Raubasine, Ajmalicin
Molecular Weight 352.43
Formula C21H24N2O3
CAS No. 483-04-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 2.5 mg/mL (7.09 mM)

TargetMolReferences and Literature

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

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Antiparasitic Natural Product Library Drug Repurposing Compound Library Approved Drug Library Selected Plant-Sourced Compound Library FDA-Approved & Pharmacopeia Drug Library Terpene Natural Product Library Natural Product Library for HTS Anti-Cancer Compound Library

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Keywords

Ajmalicine 483-04-5 GPCR/G Protein Neuroscience Adrenergic Receptor Lamuran Delta-Yohimbine Raubasine Δ-Yohimbine Ajmalicin inhibitor inhibit

 

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