Arecaidine 

Arecaidine is a GABA transport system inhibitor. Arecaidine 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 inhibits the uptake of γ-aminobutyric acid and β-alanine by the central nervous system of cats. Arecaidine inhibits hPAT1-mediated L-[³H]proline uptake in cells. Arecaidine can be used in research related to neurological diseases^[1][2][3].

Arecaidine 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) 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) 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) 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) 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) 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) competitively inhibits hPAT1-mediated uptake of L-[³H]proline in Caco-2 cells, with a K_i value of 7.3 mM^[3].
Arecaidine (0.1-100 mM; 10 min) inhibits hPAT1-mediated L-[³H]proline uptake in transiently transfected HeLa cells, with a K_i value of 3.8 mM^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Topical administration of arecaidine (1 mg/mL; once daily for 16 weeks) to the buccal mucosa induces oral submucous fibrosis in rats, which is characterized by reduced mouth opening, increased collagen deposition, elevated TGF-β expression, and dysregulated PPAR-γ signaling pathway^[1].
Arecaidine (0.2 M solution; electrophoretic) 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.

141.17

C₇H₁₁NO₂

499-04-7

Solid

White to off-white

O=C(C1=CCCN(C)C1)O

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* 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 (protect from 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.

• [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]