Ergoline-8-beta-methanol, 10-methoxy-1,6-dimethyl-, 5-bromonicotinate (ester)
nicergoline
CAS: 27848-84-6
Molecular Formula: C24H26BrN3O3
Ergoline-8-beta-methanol, 10-methoxy-1,6-dimethyl-, 5-bromonicotinate (ester) - Names and Identifiers
Ergoline-8-beta-methanol, 10-methoxy-1,6-dimethyl-, 5-bromonicotinate (ester) - Physico-chemical Properties
| Molecular Formula | C24H26BrN3O3 |
| Molar Mass | 484.39 |
| Density | 1.3558 (rough estimate) |
| Melting Point | 136-138° |
| Boling Point | 594.4±50.0 °C(Predicted) |
| Flash Point | 313.252°C |
| Water Solubility | Soluble in alcohol, chloroform, and acetone. Insoluble in water. |
| Solubility | Practically insoluble in water, freely soluble in methylene chloride, soluble in ethanol (96 per cent). |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | neat |
| Color | White to Off-White |
| Merck | 14,9496 |
| pKa | 6.33±0.40(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Refractive Index | 1.6200 (estimate) |
| In vitro study | Nicergoline (0.3-30 μM; 24 h) attenuates activated microglia- and astrocytes-induced neuronal cell death. Nicergoline (0.3-30 μM; 48 h) suppresses the production of proinflammatory cytokines and superoxide anion by activated microglia. |
Ergoline-8-beta-methanol, 10-methoxy-1,6-dimethyl-, 5-bromonicotinate (ester) - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | 22 - Harmful if swallowed |
| Safety Description | 36 - Wear suitable protective clothing. |
| UN IDs | 1544 |
| WGK Germany | 3 |
| RTECS | KE6341000 |
| HS Code | 29396100 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 in male mice, rats (mg/kg): 860, 2800 orally; 46, 43 i.v. (Neumann, Lauschner) |
Ergoline-8-beta-methanol, 10-methoxy-1,6-dimethyl-, 5-bromonicotinate (ester) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.064 ml | 10.322 ml | 20.645 ml |
| 5 mM | 0.413 ml | 2.064 ml | 4.129 ml |
| 10 mM | 0.206 ml | 1.032 ml | 2.064 ml |
| 5 mM | 0.041 ml | 0.206 ml | 0.413 ml |
Last Update：2024-01-02 23:10:35
Ergoline-8-beta-methanol, 10-methoxy-1,6-dimethyl-, 5-bromonicotinate (ester) - Reference Information
| Overview | Nicergoline is a semi-synthetic ergot alkaloid derivative. Since successful research and development in the 2060s, it has been registered and used in more than 50 countries. It has also been widely used in cerebrovascular disease, dementia, dizziness and other diseases in China. |
| mechanism of action | improving cerebral circulation: nicergoline can dilate resistance blood vessels, thereby improving cerebral circulation. As a specific adrenaline α1 receptor blocker, the drug can inhibit the pressure reflex of the resistance blood vessels, increase the local cerebral blood flow and glucose utilization rate during the reperfusion period after bilateral internal carotid artery ligation in rats; reduce the blood pressure of anesthetized dogs, but does not affect the cerebral blood flow; and can improve the cerebral vasospasm induced by experimental subarachnoid hemorrhage in rabbits. Improve brain metabolism and electrophysiological activities: Long-term treatment of nicergoline can improve the glucose utilization rate of brain extracts in aged rats. Acute medication can improve the memory function of elderly subjects, increase the total energy of EEG topography, and reduce slow waves. |
| Biological activity | Nicergoline, ergoline derivative of bromotinic acid, is an effective, selective and orally active α1A-adrenergic receptor antagonist. Nicergoline have vasodilatory effects. Nicergoline can improve the cognitive function of Alzheimer's mice. |
| Target | Value |
| Animal Model: | 3×Tg-AD mice (male, 28-35 g, 6 weeks) with the Alzheimer's disease |
| Dosage: | 10 mg/kg |
| Administration: | I.v. once daily for 60 days |
| Result: | Improved neurogenesis and cognitive competence. Decreased the degree of dementia. Downregulated pathogenic Aβ-42 and -40 peptides and APP in the hippocampi. Increased Levels of the neuroprotective forkhead box protein P2 (Foxp2), Src homology 2-containing inositol phosphatase (SxIP) and end-binding proteins (EB) in the hippocampi. Exhibited marked differences in the dispersion of the pyramidal cell layer between the nicergoline-treated and control groups. |
Last Update：2024-04-10 22:29:15
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