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| 10mg |
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| 100mg |
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Dehydroevodiamine hydrochloride, the hydrochloride salt of dehydroevodiamine, is a naturally occurring quinazoline alkaloid isolated from the unripe fruit of Evodia rutaecarpa (Rutaceae) with a variety of biological effects such as hypotensive, negative chronotropic, ion channel depressa.
| ln Vivo |
In anesthetized, spontaneously breathing cats, intravenous administration of DHE·HCl at doses of 0.1 and 0.3 mg/kg increased cerebral blood flow (CBF) recorded from the surface of the suprasylvian gyrus. The CBF response reached a maximum 1–4 minutes after injection and returned to baseline within 10 minutes. At 0.3 mg/kg, the effect was more pronounced in peak amplitude and duration compared to 0.1 mg/kg. At 0.03 mg/kg, DHE·HCl had no effect on CBF. Baseline CBF ranged from 29 to 65 ml/min/100 g tissue weight (mean 46 ± 7 ml/min/100 g, n=12). The compound had negligible effects on other cardiorespiratory functions at the doses examined. Systolic and diastolic blood pressure (baseline: 165 ± 4 mmHg and 136 ± 6 mmHg, respectively, n=12), electrocardiogram, heart rate (baseline: 207 ± 8 /min), end-tidal CO₂ concentration (baseline: 4.9 ± 0.2%), respiratory rate (baseline: 26 ± 3 /min), and inspiratory myogram of the external intercostal muscle were all unchanged. The results suggest that DHE·HCl selectively increases CBF. [1]
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| Animal Protocol |
Adult cats of either sex, weighing 2.3–3.5 kg, were initially anesthetized with halothane for cannulation of the trachea, femoral artery, and femoral vein. The head was placed in a stereotaxic frame. After intravenous injection of a mixture of α-chloralose (50 mg/kg) and urethane (200 mg/kg), halothane anesthesia was discontinued. Body temperature was maintained at 36.5–38.0°C by external heating. The skull was exposed and a 10 mm diameter hole was made on one side of the parietal region corresponding to the suprasylvian gyrus. A laser-Doppler probe was positioned epidurally to measure CBF changes using a tissue blood flowmeter. Systemic blood pressure from the femoral artery was measured with a pressure transducer. Bipolar stainless steel electrodes were inserted into the external intercostal muscle to measure inspiratory activity. Electrocardiogram (lead II) was recorded with needle electrodes, and heart rate was counted. End-tidal CO₂ concentration and respiratory rate were measured with a respiratory CO₂ monitor. Recordings were continuously displayed on a chart recorder and stored on magnetic tape. DHE·HCl was dissolved in 165 mM physiological saline solution at concentrations of 0.1 and 0.5 mg/ml and administered as a bolus dose through the femoral vein at doses of 0.03, 0.1, and 0.3 mg/kg. Quantitative data were expressed as means ± SE, and values before and after administration were evaluated using a paired t-test (p<0.05 considered significant). [1]
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| References | |
| Additional Infomation |
See also: Dehydroevodiamine chloride (preferred).
The present results are consistent with an earlier observation that isoevodiamine increased carotid blood flow without changing systemic blood pressure in anesthetized rabbits. However, the findings differ from previous reports showing hypotensive effects of dehydroevodiamine hydrochloride in anesthetized rats at doses 50–100 times larger than those used in the current study. The authors selected low doses that exclusively affect CBF without influencing other functions, supporting the contention that Evodia rutaecarpa contains a constituent that selectively increases CBF. Traditional uses of Evodia fruits (“Goshuyu”), leaves, and roots include treatment of gastrointestinal disorders, headache, migraine, and as a cardiotonic and analgesic. [1] |
| Molecular Formula |
C19H16CLN3O
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|---|---|
| Molecular Weight |
337.8028
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| Exact Mass |
337.098
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| CAS # |
111664-82-5
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| Related CAS # |
Dehydroevodiamine;67909-49-3
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| PubChem CID |
135393457
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| Appearance |
White to yellow solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
24
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| Complexity |
753
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C2=CC=CC=C2C(=O)N3C1=C4C(=C5C=CC=CC5=N4)CC3.Cl
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| InChi Key |
SVOMSEHNGXLQRU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H15N3O.ClH/c1-21-16-9-5-3-7-14(16)19(23)22-11-10-13-12-6-2-4-8-15(12)20-17(13)18(21)22;/h2-9H,10-11H2,1H3;1H
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| Chemical Name |
21-methyl-3,13,21-triazapentacyclo[11.8.0.02,10.04,9.015,20]henicosa-1,3,5,7,9,15,17,19-octaen-14-one;hydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~12.5 mg/mL (~37.00 mM)
H2O : ~1.43 mg/mL (~4.23 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.70 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 12.5 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: ≥ 1.25 mg/mL (3.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9603 mL | 14.8017 mL | 29.6033 mL | |
| 5 mM | 0.5921 mL | 2.9603 mL | 5.9207 mL | |
| 10 mM | 0.2960 mL | 1.4802 mL | 2.9603 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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