| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Arecaidine primarily targets the GABA transporter, functioning as a potent GABA reuptake inhibitor. By inhibiting GABA reuptake, it enhances GABAergic inhibition in the central nervous system. Additionally, Arecaidine is a substrate of the H+-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake. Its primary proposed mechanisms are the inhibition of GABA uptake and its role as a PAT1 substrate.
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| ln Vitro |
In vitro, Arecaidine inhibits GABA uptake and enhances GABAergic inhibition. It acts as a potent GABA reuptake inhibitor and is a substrate of PAT1, competitively inhibiting L-proline uptake. The compound displays structural similarity to other GABA uptake inhibitors. These in vitro activities confirm its role as a modulator of inhibitory neurotransmission and amino acid transport.
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| ln Vivo |
In vivo, Arecaidine has demonstrated sedative effects in murine models and protective activity against lethality induced by GABAA receptor antagonists. However, studies in cats and mice show that while Arecaidine inhibits GABA uptake and enhances GABAergic inhibition in vitro, it shows minimal anticonvulsant or synaptic inhibitory effects in vivo, even at doses up to 1 g/kg. This suggests limited in vivo efficacy for central nervous system modulation.
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| Enzyme Assay |
The GABA reuptake inhibitory activity is assessed using in vitro assays with brain slices or synaptosomes. Arecaidine is incubated with tissue preparations and radiolabeled GABA, and the amount of GABA taken up is measured by scintillation counting. PAT1 transporter activity is evaluated using cell-based uptake assays with radiolabeled L-proline or other substrates. The compound's ability to inhibit GABA uptake and compete with proline is determined from dose-response curves.
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| Cell Assay |
For cellular studies, neuronal cell lines or primary neuronal cultures are used. Cells are treated with Arecaidine at various concentrations, and GABA uptake is measured using radiolabeled GABA or fluorescent GABA analogs. PAT1-mediated transport is assessed in cells expressing the transporter. Cell viability is assessed using standard assays. The compound is soluble in water at 200 mg/mL (1416.73 mM).
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| Animal Protocol |
In vivo studies for Arecaidine have been conducted in cats and mice. The compound was administered intravenously, topically, or subcutaneously at doses up to 1 g/kg. In murine models, sedative effects and protection against GABAA receptor antagonist-induced lethality were assessed. However, minimal anticonvulsant or synaptic inhibitory effects were observed in vivo. Specific protocols for behavioral or electrophysiological assessments are not detailed in the available literature.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for Arecaidine are not extensively reported. The compound has a molecular weight of 141.17 g/mol and is highly soluble in water (200 mg/mL, 1416.73 mM). It is stable as a powder at -20°C for up to 3 years or in solvent at -80°C for 1 year. Pharmacokinetic studies would be required to determine parameters such as absorption, distribution, metabolism, and excretion in animal models.
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| Toxicity/Toxicokinetics |
Toxicological data for Arecaidine are limited. As an alkaloid from areca nuts, which are known to have carcinogenic potential when chewed, the compound should be handled with caution. In animal studies, doses up to 1 g/kg were administered, but comprehensive toxicology data are not available. The compound's effects on GABAergic and amino acid transport systems warrant careful evaluation. It should be handled with appropriate safety precautions in laboratory settings.
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| References |
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| Additional Infomation |
Arecoline is a citrate compound. It has been reported to be found in areca nut (Areca catechu), and relevant data exists. See also: Arecoline hydrochloride (note moved here).
Arecaidine is a pyridine alkaloid from areca nuts that acts as a potent GABA reuptake inhibitor and PAT1 substrate. It shows sedative effects in murine models and is used in neuropharmacological research. Despite its in vitro activity, it shows minimal anticonvulsant effects in vivo. No clinical trials or regulatory approvals exist. For research use only. |
| Molecular Formula |
C7H11NO2
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|---|---|
| Molecular Weight |
141.1677
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| Exact Mass |
141.078
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| CAS # |
499-04-7
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| Related CAS # |
Arecaidine hydrochloride;6018-28-6;Arecaidine hydrobromide;6013-57-6
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| PubChem CID |
10355
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
266.7±35.0 °C at 760 mmHg
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| Melting Point |
232ºC (dec.)
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| Flash Point |
115.1±25.9 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.524
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| LogP |
0.77
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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 |
1
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| Heavy Atom Count |
10
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| Complexity |
174
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DNJFTXKSFAMXQF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H11NO2/c1-8-4-2-3-6(5-8)7(9)10/h3H,2,4-5H2,1H3,(H,9,10)
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| Chemical Name |
1-methyl-3,6-dihydro-2H-pyridine-5-carboxylic acid
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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) |
H2O : ~250 mg/mL (~1770.91 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (708.37 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 7.0837 mL | 35.4183 mL | 70.8366 mL | |
| 5 mM | 1.4167 mL | 7.0837 mL | 14.1673 mL | |
| 10 mM | 0.7084 mL | 3.5418 mL | 7.0837 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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