Arecaidine hydrobromide
Based on 1 publication(s) in Google Scholar
Arecaidine hydrobromide is a GABA transport system inhibitor. Arecaidine hydrobromide inhibits the proliferation of oral mucosal fibroblasts, increases the secretion of IL-6, TGF-β and TNF-α in cells, downregulates the expression of PPAR-γ and PCK1 in cells, and upregulates the expression of TGF-β1. Arecaidine hydrobromide inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine hydrobromide inhibits hPAT1-mediated L-[3H]proline uptake in cells. Arecaidine hydrobromide can be used in research related to neurological diseases.
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- Reinheit: 98.0%
- CAS. Nr.: 6013-57-6
- Formel: C7H12BrNO2
- Molecular Weight:222.08
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Arecaidine hydrobromide
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Biologische Aktivität
Beschreibung
In Vitro
Arecaidine hydrobromide exhibits strong binding affinity for PPAR-γ, PCK1 and TGF-β1 proteins, with binding energies of -5.1 kJ/mol, -5.6 kJ/mol and -5.6 kJ/mol[1].
Arecaidine (0-120 μg/mL; 24-48 h) hydrobromide inhibits the proliferation of human oral mucosal fibroblasts (hOMF) and increases the secretion of IL-6, TGF-β and TNF-α in cells[1].
Arecaidine (100-120 μg/mL; 48 h) hydrobromide downregulates the mRNA and protein expression of PPAR-γ and PCK1, while upregulates the mRNA and protein expression of TGF-β1, in human oral mucosal fibroblasts (hOMF)[1].
Arecaidine (10 min) hydrobromide inhibits the uptake of GABA and β-alanine, but not that of glycine, in cat spinal cord slices, with an IC50 of 89 μM for GABA and 193 μM for β-alanine[2].
Arecaidine (10 min) hydrobromide inhibits the uptake of GABA and β-alanine in cat cerebellar slices, with an IC50 value of 76 μM for GABA and 354 μM for β-alanine[2].
Arecaidine (10 min) hydrobromide inhibits the uptake of GABA and β-alanine in rat cerebral cortex slices, with an IC50 value of 122 μM for GABA and 208 μM for β-alanine[2].
Arecaidine (0.1-100 mM; 10 min) hydrobromide competitively inhibits hPAT1-mediated uptake of L-[3H]proline in Caco-2 cells, with a Ki value of 7.3 mM[3].
Arecaidine (0.1-100 mM; 10 min) hydrobromide inhibits hPAT1-mediated L-[3H]proline uptake in transiently transfected HeLa cells, with a Ki value of 3.8 mM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human oral mucosal fibroblasts (hOMF)
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Concentration:0, 40, 60, 80, 100, 120 μg/mL
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Incubation Time:24 h; 48 h
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Result:Did not significantly alter hOMF cell viability after 24 h of treatment across all tested concentrations.
Significantly inhibited hOMF cell proliferation at 100 μg/mL and 120 μg/mL after 48 h of treatment.
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Cell Line:human oral mucosal fibroblasts (hOMF)
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Concentration:100, 120 μg/mL
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Incubation Time:48 h
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Result:Significantly elevated IL-6, TGF-β, TNF-α levels.
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Cell Line:human oral mucosal fibroblasts (hOMF)
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Concentration:100, 120 μg/mL
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Incubation Time:48 h
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Result:Significantly downregulated PPAR-γ, PCK1, TGF-β1 mRNA expression.
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Cell Line:human oral mucosal fibroblasts (hOMF)
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Concentration:100 μg/mL
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Incubation Time:48 h
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Result:Significantly reduced PPAR-γ, PCK1, TGF-β1 protein expression.
In Vivo
Arecaidine (0.2 M solution; electrophoretic) hydrobromide selectively potentiates the inhibitory effects of GABA and β-alanine on cat spinal cord neurons, and enhances the effect of GABA on cat cerebellar Purkinje cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male, 6-8 weeks old, 200 g)[1]
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Dosage:1 mg/mL
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Administration:topical application to buccal mucosa; once daily; 16 weeks
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Result:Reduced passive mouth opening to 23.97 mm, a statistically significant reduction compared to the control group.
Increased collagen volume fraction significantly higher than the control group.
Increased TGF-β protein expression statistically significantly compared to the control group.
Identified 100 significantly differentially expressed genes, including downregulation of PPAR-γ, PCK1, pdk4, plin5, Hmgcs2, UCP3, and Angptl4, and upregulation of TGF-β1 and FOS.
Demonstrated binding energies < -5.0 kJ/mol with PPAR-γ, PCK1, and TGF-β1, indicating strong binding affinity.
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Animal Model:unspecified strain (anaesthetised with pentobarbitone sodium)[2]
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Dosage:0.2M solution
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Administration:electrophoretic; variable duration
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Result:Selectively potentiated the inhibitory effects of GABA and β-alanine on cat spinal cord neurons, and enhanced the effect of GABA on cat cerebellar Purkinje cells.
Chemical Information
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CAS. Nr. 6013-57-6
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Appearance Solid
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Molecular Weight 222.08
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Formel C7H12BrNO2
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Color White to off-white
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SMILES
O=C(C1=CCCN(C)C1)O.[H]Br
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Mol Sci
Oxidative Stress and Endoplasmic Reticulum Stress Contributes to Arecoline and Its Secondary Metabolites-Induced Dyskinesia in Zebrafish Embryos. [Abstract]2023 Mar 28;24(7):6327. PMID: 37047326
Lösungsmittel & Löslichkeit
In Vitro:
H2O : 100 mg/mL (450.29 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (289 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Zeng F, et al. Inhibitory role of arecaidine on PPARγ signaling in oral mucosa: Mechanistic insights from transcriptome and experimental analysis. Toxicon. 2025;262:108403. [Content Brief]
[2]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977;136(3):513-522. [Content Brief]
[3]. Voigt V, et al. Transport of the areca nut alkaloid arecaidine by the human proton-coupled amino acid transporter 1 (hPAT1). J Pharm Pharmacol. 2013;65(4):582-590. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 4.5029 mL | 22.5144 mL | 45.0288 mL | 112.5720 mL |
| 5 mM | 0.9006 mL | 4.5029 mL | 9.0058 mL | 22.5144 mL | |
| 10 mM | 0.4503 mL | 2.2514 mL | 4.5029 mL | 11.2572 mL | |
| 15 mM | 0.3002 mL | 1.5010 mL | 3.0019 mL | 7.5048 mL | |
| 20 mM | 0.2251 mL | 1.1257 mL | 2.2514 mL | 5.6286 mL | |
| 25 mM | 0.1801 mL | 0.9006 mL | 1.8012 mL | 4.5029 mL | |
| 30 mM | 0.1501 mL | 0.7505 mL | 1.5010 mL | 3.7524 mL | |
| 40 mM | 0.1126 mL | 0.5629 mL | 1.1257 mL | 2.8143 mL | |
| 50 mM | 0.0901 mL | 0.4503 mL | 0.9006 mL | 2.2514 mL | |
| 60 mM | 0.0750 mL | 0.3752 mL | 0.7505 mL | 1.8762 mL | |
| 80 mM | 0.0563 mL | 0.2814 mL | 0.5629 mL | 1.4072 mL | |
| 100 mM | 0.0450 mL | 0.2251 mL | 0.4503 mL | 1.1257 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Arecaidine hydrobromide Related Classifications
HY-N2368B Related Classifications
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