Arecoline

Arecoline, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress^{[1][2][3][4][5]}. IC50 & Target:nAChR/mAChR^[3] In Vitro: Arecoline induces the generation of reactive oxygen species and cell cycle arrest at the G1/G0 phase in HaCaT cells without affecting the expression of p21/Cip1. Arecoline-induced epithelial cell death at higher concentrations is caused by oxidative trauma without eliciting apoptosis. Arecoline upregulates the expression of the following stress-responsive genes: hemeoxygenase-1; ferritin light chain; glucose-6-phosphate dehydrogenase; glutamatecysteine ligase catalytic subunit; and glutathione reductase^[1]. In Vivo: Arecoline (0.2% in water; p.o., 2 weeks) alleviates the anxiety and depression in CFA (HY-153808)-induced mice^[5].