| Size | Price | |
|---|---|---|
| 100mg | ||
| Other Sizes |
| Targets |
Noreleagnine targets the serotonin transporter and the 5-HT2A receptor. As a competitive serotonin reuptake inhibitor with a Ki of 6.1 µM, it blocks the reuptake of serotonin, increasing serotonin levels in the synaptic cleft. It also targets the 5-HT 2A receptor (HTR2A) as an inhibitor. This dual mechanism of action on serotonergic signaling makes it relevant for studying mood disorders, neurodegenerative diseases, and cancer. Its role as a mitotic kinesin inhibitor suggests additional targets related to cell division.
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| ln Vitro |
In vitro, Noreleagnine has been characterized as a competitive serotonin reuptake inhibitor with a Ki of 6.1 µM. It targets the 5-HT 2A receptor as an inhibitor. It is used in the study of neurodegenerative diseases. Its activity as a mitotic kinesin inhibitor suggests potential anticancer activity. These in vitro activities confirm its potential for research on serotonergic signaling, neurodegenerative diseases, and cancer.
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| ln Vivo |
Serotonin levels are raised in the same area of the rat brain by tetrahydro-beta-carboline (20 µg; icv) [1].
In vivo studies of Noreleagnine are not extensively documented. As a serotonin reuptake inhibitor and 5-HT2A receptor inhibitor, it may have effects on mood, behavior, and neurological function. Its potential as a mitotic kinesin inhibitor suggests possible anticancer activity in vivo. However, comprehensive in vivo efficacy and safety data are limited. The compound is primarily used in research applications. Further studies are needed to fully characterize its in vivo biological activity and therapeutic potential. |
| Enzyme Assay |
For in vitro biochemical assays, Noreleagnine is evaluated for its serotonin reuptake inhibitory activity and receptor binding. Serotonin reuptake inhibition is measured using assays with synaptosomes or cells expressing the serotonin transporter, determining Ki values (6.1 µM). 5-HT2A receptor binding is assessed using radioligand competition binding assays with membrane preparations from cells expressing the receptor. Kinesin inhibition is assessed using enzyme activity assays. These cell-free and cell-based assays help characterize the compound's multiple biological activities.
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| Cell Assay |
In vitro cellular assays for Noreleagnine are performed using various cell types including neuronal cells, cancer cells, and cells expressing serotonin transporters or 5-HT2A receptors. Cells are cultured in standard media and treated with the compound at various concentrations. Serotonin uptake is measured using radiolabeled serotonin. Receptor binding is assessed using radioligand binding assays. Cell viability and proliferation are assessed using MTT or SRB assays. These cellular assays help validate the compound's serotonin reuptake inhibitory, receptor binding, and anticancer activities.
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| Animal Protocol |
Animal/Disease Models: 180-200g female SD (SD (Sprague-Dawley)) rats [1]
Doses: 20 µg Route of Administration: intracerebroventricular injection Experimental Results: Serotonin levels increased in the same part of the brain, while monoamine oxidase activity did not change. In vivo animal experiments with Noreleagnine are not extensively documented. As a serotonin reuptake inhibitor and 5-HT2A receptor inhibitor, it could be studied in models of depression, anxiety, or neurodegenerative diseases. Its potential as a mitotic kinesin inhibitor suggests possible anticancer studies. Administration routes would include oral gavage, intraperitoneal injection, or intravenous injection. Researchers should consult the primary literature for any available in vivo protocols and data. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Noreleagnine are not extensively documented. As a small molecule with a molecular weight of 172.23, it is expected to have good oral bioavailability and tissue distribution, including penetration of the blood-brain barrier. Detailed PK parameters such as half-life, Cmax, Tmax, AUC, and protein binding are not available in the literature. The compound should be stored under recommended conditions to maintain stability.
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| Toxicity/Toxicokinetics |
The toxicological profile of Noreleagnine is not extensively characterized. As a natural alkaloid related to tryptamines, it may have dose-dependent toxicity at high concentrations. The compound is intended for research use only and not for human therapeutic applications. Comprehensive toxicity studies including acute, subchronic, and chronic toxicity assessments are limited. Researchers should follow standard laboratory safety practices when handling Noreleagnine.
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| References | |
| Additional Infomation |
2,3,4,9-Tetrahydro-1H-pyrido[3,4-b]indole belongs to the β-carboline class of compounds. It has been reported that the blue tiger fly contains tryptophan, and relevant data exists.
Noreleagnine is a valuable research tool for studying serotonergic signaling, neurodegenerative diseases, and cancer. Its competitive serotonin reuptake inhibition (Ki = 6.1 µM) makes it useful for investigating the role of serotonin in mood disorders and neurological function. Its 5-HT2A receptor inhibition provides opportunities for studying this receptor's role in various physiological and pathological processes. Its potential as a mitotic kinesin inhibitor makes it relevant for cancer research. As a tryptoline alkaloid, it is also important for natural product chemistry research. |
| Molecular Formula |
C11H12N2
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|---|---|
| Molecular Weight |
172.2264
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| Exact Mass |
172.1
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| Elemental Analysis |
C, 76.71; H, 7.02; N, 16.27
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| CAS # |
16502-01-5
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| Related CAS # |
58911-02-7 (mono-hydrochloride)
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| PubChem CID |
107838
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| Appearance |
Light brown to brown solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
351.6±32.0 °C at 760 mmHg
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| Melting Point |
206-208 °C(lit.)
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| Flash Point |
166.5±25.1 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.670
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| LogP |
1.33
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
13
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| Complexity |
193
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1([H])C2=C([H])C([H])=C([H])C([H])=C2C2C([H])([H])C([H])([H])N([H])C([H])([H])C1=2
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| InChi Key |
CFTOTSJVQRFXOF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H12N2/c1-2-4-10-8(3-1)9-5-6-12-7-11(9)13-10/h1-4,12-13H,5-7H2
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| Chemical Name |
2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
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| Synonyms |
Tetrahydronorharman; Tryptoline; Tetrahydro-β-carboline; 1,2,3,4-Tetrahydro-β-carboline; THBC
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 (~580.62 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.8062 mL | 29.0309 mL | 58.0619 mL | |
| 5 mM | 1.1612 mL | 5.8062 mL | 11.6124 mL | |
| 10 mM | 0.5806 mL | 2.9031 mL | 5.8062 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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