| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
α1A-adrenoceptor
Nicergoline targets α₁-adrenergic receptors, acting as an antagonist. It also has effects on dopamine and serotonin receptors. By blocking α₁-adrenergic receptors, it causes vasodilation and improves blood flow. Nicergoline also has metabolic effects, improving glucose utilization and oxygen consumption in the brain. Its multi-modal mechanism contributes to its cognitive-enhancing effects. |
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| ln Vitro |
Nicergoline (0.3-30 μM; 24 h) reduces the amount of neuronal cell death caused by astrocytes and activated microglia[3].
Nicergoline (0.3-30 μM; 48 h) inhibits activated microglia's generation of proinflammatory cytokines and superoxide anion[3]. In vitro, Nicergoline is an α₁-adrenergic receptor antagonist. Its binding affinity for α₁-adrenergic, dopamine, and serotonin receptors has been characterized. It has been shown to have neuroprotective effects in cell-based assays. Nicergoline also inhibits platelet aggregation. |
| ln Vivo |
Nicergoline (10 mg/kg; i.v. once daily for 60 d) improves impaired neurogenesis and cognitive function in mice with Alzheimer's disease[2].
Nicergoline (10 mg/kg; intravenously once daily for 60 days) inhibits oxidative stress, inflammation, and apoptosis in hippocampus cells and controls hippocampus cell activity via the PI3K/AKT signaling pathway in mice[2]. In vivo, Nicergoline has been shown to improve cognitive function in patients with dementia and cognitive decline. It improves cerebral blood flow and has neuroprotective effects. Nicergoline is used clinically for the treatment of cerebrovascular disorders and age-related cognitive impairment. It is an orally active compound. |
| Enzyme Assay |
The activity of Nicergoline can be assessed using radioligand binding assays. Membranes prepared from tissues expressing α₁-adrenergic receptors are incubated with a radiolabeled α₁-adrenergic ligand and varying concentrations of Nicergoline. The displacement of the radioligand is measured to determine the binding affinity (IC₅₀ or Ki). Functional assays measuring α₁-adrenergic receptor-mediated signaling can also be used.
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| Cell Assay |
To evaluate the cellular effects of Nicergoline, neuronal cells or vascular smooth muscle cells are treated with the compound. The inhibition of α₁-adrenergic receptor-mediated signaling is measured. The effects on cell viability, neuroprotection, and inflammation are assessed. Its effects on platelet aggregation are evaluated using platelet-rich plasma.
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| Animal Protocol |
3×Tg-AD mice (male, 28-35 g, 6 weeks) with the Alzheimer's disease
10 mg/kg I.v. once daily for 60 days In vivo studies with Nicergoline typically involve administration to animal models via oral routes. In models of cognitive impairment, the compound's effects on learning, memory, and neuroinflammation are assessed. Its effects on cerebral blood flow and neuroprotection are also evaluated. Pharmacokinetic parameters, such as oral bioavailability and brain penetration, are characterized. |
| ADME/Pharmacokinetics |
Nicergoline has a molecular formula of C₂₄H₂₆BrN₃O₃ and a molecular weight of 484.39 g/mol. Its CAS number is 27848-84-6. It is a semisynthetic ergot alkaloid derivative. It is soluble in DMSO and other organic solvents. The purity is typically >98%. It should be stored according to the manufacturer's instructions.
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| Toxicity/Toxicokinetics |
Nicergoline is generally well-tolerated but can cause side effects such as hypotension, dizziness, and gastrointestinal disturbances. It is contraindicated in patients with severe bradycardia, recent myocardial infarction, or hypersensitivity to ergot alkaloids. It should be used with caution in patients with hepatic or renal impairment.
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| References |
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| Additional Infomation |
Nicergoline is an organic nitrogen heterocyclic compound and an organic heterotetracyclic compound. It is an ergot derivative and has been used as a cerebral vasodilator and to treat peripheral vascular disease. Studies have shown that it can improve cognitive impairment in patients with cerebrovascular disease. It is an ergot derivative and has been used as a cerebral vasodilator and to treat peripheral vascular disease. It may improve cognitive impairment in patients with cerebrovascular disease. Indications: Used to treat Alzheimer's disease, vascular migraine, transient ischemic attack, increased platelet aggregation, and macular degeneration. Mechanism of Action: Nicergoline acts by inhibiting postsynaptic α1-adrenergic receptors on vascular smooth muscle. This inhibits the vasoconstrictive effects of circulating and locally released catecholamines (adrenaline and noradrenaline), leading to peripheral vasodilation. Therefore, the mechanism of action of nicergoline is to increase cerebral circulation, thereby enhancing the transmission of nerve signals along nerve fibers that secrete acetylcholine (a neurotransmitter).
Pharmacodynamics Nicergoline is a potent vasodilator (improves cerebral blood flow). In the brain, it reduces vascular resistance, increases arterial blood flow, and stimulates the utilization of oxygen and glucose. Nicergoline also improves blood circulation in the lungs and limbs and has been shown to inhibit platelet aggregation. Nicergoline is a semisynthetic ergot alkaloid derivative used for the treatment of cognitive decline and dementia. It acts as an α₁-adrenergic receptor antagonist and has vasodilatory and metabolic effects. Nicergoline improves cerebral blood flow and cognitive function. It is a research tool for studying cognitive disorders and vascular dementia. |
| Molecular Formula |
C24H26BRN3O3
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|---|---|
| Molecular Weight |
484.3855
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| Exact Mass |
483.115
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| Elemental Analysis |
C, 59.51; H, 5.41; Br, 16.50; N, 8.67; O, 9.91
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| CAS # |
27848-84-6
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| Related CAS # |
Nicergoline-13C,d3
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| PubChem CID |
34040
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
594.4±50.0 °C at 760 mmHg
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| Melting Point |
136-138°
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| Flash Point |
313.3±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
4.34
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
681
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| Defined Atom Stereocenter Count |
3
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| SMILES |
BrC1=C([H])N=C([H])C(=C1[H])C(=O)OC([H])([H])[C@@]1([H])C([H])([H])N(C([H])([H])[H])[C@]2([H])C([H])([H])C3=C([H])N(C([H])([H])[H])C4=C([H])C([H])=C([H])C(=C34)[C@]2(C1([H])[H])OC([H])([H])[H]
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| InChi Key |
YSEXMKHXIOCEJA-FVFQAYNVSA-N
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| InChi Code |
InChI=1S/C24H26BrN3O3/c1-27-13-17-8-21-24(30-3,19-5-4-6-20(27)22(17)19)9-15(12-28(21)2)14-31-23(29)16-7-18(25)11-26-10-16/h4-7,10-11,13,15,21H,8-9,12,14H2,1-3H3/t15-,21-,24+/m1/s1
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| Chemical Name |
[(6aR,9R,10aS)-10a-methoxy-4,7-dimethyl-6a,8,9,10-tetrahydro-6H-indolo[4,3-fg]quinolin-9-yl]methyl 5-bromopyridine-3-carboxylate
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| Synonyms |
Nicergoline; Sermion; Nicotergoline; Nimergoline
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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: 22~100 mg/mL (45.4~206.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.16 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 25.0 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: ≥ 2.5 mg/mL (5.16 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 25.0 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 | 2.0645 mL | 10.3223 mL | 20.6445 mL | |
| 5 mM | 0.4129 mL | 2.0645 mL | 4.1289 mL | |
| 10 mM | 0.2064 mL | 1.0322 mL | 2.0645 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05551182 | Not yet recruiting | Drug: Nicergoline | Dysphagia | Phramongkutklao College of Medicine and Hospital |
January 2023 | Phase 3 |
| NCT04176367 | Completed | Drug: Nicergoline from China Drug: Nicergoline from Italy |
Pharmacokinetics | Pfizer's Upjohn has merged with Mylan to form Viatris Inc. |
December 17, 2019 | Phase 1 |
| NCT01009476 | Completed | Drug: Galantamine Drug: Nootropics (ginkgo biloba, nicergoline, piracetam, or others) |
Dementia Alzheimer Disease Dementia, Vascular |
Janssen-Cilag G.m.b.H | March 2006 | N/A |
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