| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Raubasine primarily targets the alpha-1 (α1) adrenoceptor, which it blocks preferentially over the alpha-2 (α2) adrenoceptor. By blocking α1-adrenergic receptors, it induces vasodilation and lowers peripheral vascular resistance, thereby reducing blood pressure. It also acts as a reversible but non-competitive nicotine receptor antagonist with an IC50 of 72.3 µM.
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|---|---|
| ln Vitro |
α1-adrenergic receptors are preferentially blocked by ajmalicine, as opposed to α2-adrenergic receptors [1]. In a concentration-dependent manner, ajmalicine inhibits contraction (IC50=72.3 ± 22.5 μM)[2]. Ajmalicine operates preferentially on the postsynaptic site, with a pA2 value of 6.2[3] indicating that it blocks the inhibitory action of clonidine and competitively antagonizes the effect of norepinephrine on postsynaptic α-adrenergic receptors.
In vitro, Raubasine's activity is characterized by its binding affinity to α1-adrenoceptors. It is a potent adrenolytic agent, and its receptor binding profile is well-studied. Its activity as a nicotine receptor antagonist is also observed in vitro. |
| ln Vivo |
Ajmalicine is active on sympathetic stimulation and inhibits the pressor impact of electrical stimulation [1]. A substantial dose-dependent reduction of the pressor response to norepinephrine is produced by ajmalicine (0.5–4 mg/kg) [1].
In vivo, Raubasine functions primarily as an antihypertensive agent. Its vasodilatory effect, resulting from α1-adrenoceptor blockade, leads to a decrease in blood pressure. It also enhances cerebral blood flow, which is beneficial in certain cerebrovascular conditions. |
| Enzyme Assay |
The affinity of Raubasine for its receptors is assessed in radioligand binding assays. In these cell-free experiments, membrane preparations from tissues or cells expressing the α1-adrenoceptor are incubated with a radiolabeled antagonist. The displacement of this ligand by Raubasine is measured to determine its Ki.
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| Cell Assay |
For cellular assays, the functional antagonism of Raubasine at the α1-adrenoceptor can be studied using cell lines that express this receptor. The compound's ability to inhibit agonist-induced calcium mobilization or other downstream signals is measured.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rat (300-350 g) [1]
Doses: 0.5, 1, 2 and 4 mg/kg Route of Administration: intravenous (iv) (iv)injection, once Experimental Results: Significant pressor response to norepinephrine dose-dependent inhibition. In vivo studies for Raubasine are typically performed in animal models of hypertension, such as spontaneously hypertensive rats. The compound is administered, and its effect on blood pressure is monitored over time to confirm its antihypertensive efficacy. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Raubasine are characteristic of an alkaloid. Its absorption, distribution, metabolism, and excretion profile has been studied in animal models.
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| Toxicity/Toxicokinetics |
The toxicity of Raubasine is related to its pharmacological effect of lowering blood pressure. Overdose can lead to severe hypotension and bradycardia. As an adrenolytic agent, it can also cause sedation.
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| References |
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| Additional Infomation |
Ajmalicine is a monoterpenoid indole alkaloid with the molecular formula C21H24N2O3, isolated from various plants in the genera Rauvolfia and Catharanthus. It is a selective α1-adrenergic receptor antagonist used to treat hypertension. It possesses antihypertensive, α-adrenergic antagonistic, and vasodilatory effects. Ajmalicine is a monoterpenoid indole alkaloid, belonging to the methyl ester class of compounds, and is also an organic heteropentacyclic compound. It is the conjugate base of Ajmalicine (1+). It has been reported that Ajmalicine is present in Rauvolfia yunnanensis, Campsis grandiflora, and other organisms with relevant data.
Raubasine (Ajmalicine) is a naturally occurring alkaloid that has been used clinically as an antihypertensive agent. It is also known by various synonyms including delta-yohimbine and lamuran. Its use highlights the therapeutic potential of natural products in cardiovascular medicine. |
| Molecular Formula |
C21H24N2O3
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|---|---|
| Molecular Weight |
352.4269
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| Exact Mass |
352.178
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| CAS # |
483-04-5
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| Related CAS # |
Ajmalicine hydrochloride;4373-34-6
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| PubChem CID |
441975
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
524.0±50.0 °C at 760 mmHg
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| Melting Point |
258°C (rough estimate)
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| Flash Point |
270.7±30.1 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.656
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| LogP |
2.88
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
26
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| Complexity |
606
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C[C@H]1[C@H]2CN3CCC4=C([C@@H]3C[C@@H]2C(=CO1)C(=O)OC)NC5=CC=CC=C45
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| InChi Key |
GRTOGORTSDXSFK-XJTZBENFSA-N
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| InChi Code |
InChI=1S/C21H24N2O3/c1-12-16-10-23-8-7-14-13-5-3-4-6-18(13)22-20(14)19(23)9-15(16)17(11-26-12)21(24)25-2/h3-6,11-12,15-16,19,22H,7-10H2,1-2H3/t12-,15-,16+,19-/m0/s1
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| Chemical Name |
methyl (1S,15R,16S,20S)-16-methyl-17-oxa-3,13-diazapentacyclo[11.8.0.02,10.04,9.015,20]henicosa-2(10),4,6,8,18-pentaene-19-carboxylate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5.56 mg/mL (~15.78 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.56 mg/mL (1.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8374 mL | 14.1872 mL | 28.3744 mL | |
| 5 mM | 0.5675 mL | 2.8374 mL | 5.6749 mL | |
| 10 mM | 0.2837 mL | 1.4187 mL | 2.8374 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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