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]. In Vitro: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]. In Vivo: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].