| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Ergoloid mesylates have a complex and multifaceted mechanism of action, involving interactions with multiple receptors and neurotransmitter systems. They bind with high affinity to the GABAA receptor Cl⁻ channel, producing an allosteric interaction with the benzodiazepine site. The substance produces a generalized peripheral vasodilation and a fall in arterial pressure. It is also a α-adrenergic blocker.
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| ln Vitro |
In vitro, ergoloid mesylates bind with high affinity to the GABAA receptor Cl⁻ channel, producing an allosteric interaction with the benzodiazepine site. The mixture's components interact with multiple neurotransmitter receptors, contributing to its complex pharmacological profile. Its activity can be assessed using radioligand binding assays on various receptor preparations.
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| ln Vivo |
In vivo, ergoloid mesylates have been used to treat symptoms of mild to moderate impairment of mental function in the elderly. The substance produces a generalized peripheral vasodilation and a fall in arterial pressure. It has been used to combat decreased mental function as a result of senility or multiple small strokes. The drug is contraindicated in patients with psychosis.
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| Enzyme Assay |
Non-cellular receptor binding assays for ergoloid mesylates involve competitive radioligand binding displacement studies using membrane preparations from brain tissue expressing GABAA receptors or other targets. Membranes are incubated with a radiolabeled ligand (e.g., [³H]flunitrazepam for the benzodiazepine site) and varying concentrations of ergoloid mesylates. Binding displacement curves are generated to determine IC₅₀ values. The compound's affinity for multiple receptors can be assessed in this manner.
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| Cell Assay |
In vitro cellular assays for ergoloid mesylates are not standard, as it is a mixture of alkaloids with complex pharmacology. Its effects on neuronal function can be assessed using electrophysiological techniques, such as patch-clamp recordings on neurons, to measure its modulation of GABAA receptor-mediated currents or other ion channel activities. Its effects on neurotransmitter release can be assessed in synaptosome preparations.
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| Animal Protocol |
In vivo animal experiments with ergoloid mesylates are conducted in rodent models of cognitive impairment. Animals are treated with ergoloid mesylates via oral or intraperitoneal administration, and cognitive function is assessed using behavioral tests such as the Morris water maze, novel object recognition, and passive avoidance tests. The compound's effects on cerebral blood flow and vascular function are also assessed in these models.
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| ADME/Pharmacokinetics |
Ergoloid mesylates have a molecular weight of approximately 659.84 (for the mixture) and a molecular formula that varies by component. The mixture is a solid powder with a purity of ≥98%. It is typically stored at room temperature, protected from light and moisture. The compound is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Ergoloid mesylates are generally well-tolerated, but they can cause side effects such as nausea, gastrointestinal disturbances, and hypotension. The drug is contraindicated in patients with psychosis. It should be used with caution in patients with cardiovascular disease. Standard safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Ergoloid Mesylates (Dihydroergotoxine Mesylate; CAS 8067-24-1) is a mixture of dihydrogenated ergot alkaloids used to treat symptoms of mild to moderate impairment of mental function in the elderly. It binds with high affinity to the GABAA receptor and produces peripheral vasodilation. The compound is marketed as Hydergine and is available from various commercial suppliers for research applications.
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| Molecular Formula |
C19H25N3O2.CH4O3S
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|---|---|
| Molecular Weight |
423.53
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| CAS # |
8067-24-1
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| Related CAS # |
8067-24-1;
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| Appearance |
White to off-white solid powder
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| Density |
1.34g/cm3
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| Boiling Point |
899.5ºC at 760 mmHg
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| Flash Point |
497.8ºC
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| Index of Refraction |
1.66
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| LogP |
2.538
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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, avoid exposure to moisture. |
| 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 : ≥ 100 mg/mL H2O : ~2 mg/mL
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (Infinity 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 20.8 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: ≥ 2.08 mg/mL (Infinity 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3611 mL | 11.8055 mL | 23.6111 mL | |
| 5 mM | 0.4722 mL | 2.3611 mL | 4.7222 mL | |
| 10 mM | 0.2361 mL | 1.1806 mL | 2.3611 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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