Nine compounds were isolated from the under-ground part of Notopterygium forbesii. On the basis of physicochemical properties and spectroscopic analysis, they were identified as phellopterin, isoimperattorin, notopterol, nodakenitin, nodakenin, 6-O-trans-feruoylnodakenin, p-hydroxyphenethyl anisate, pregnenolone and beta-sitosteroi, of which phellopterin was obtained from the plant of Notopterygium genus for the first time. Bioactivity-guided fractionation of Notopterygiumforbesii has resulted in the isolation of one new coumarin glycoside and one new phenethyl vanillate, together with seventeen known compounds.The structures of these compounds were characterized by spectroscopic methods. These compounds were evaluated for their binding affinities to the opioid and dopamine receptors, and falcarindiol showed weak binding affinities to opioid receptors and moderate affinity for D1 receptor (Ki = 192 ± 6 nM).