Zanthoxylum tessmannii (Engl.) Ayafor is an important medicinal plant with roots used as a chewing stick, which are commercially available and highly pungent. A previous study identified lupeol, fagaramide, nitidine, chelerythrine, and fagaridine in its roots, with nitidine shown to lower rabbits' diastolic and systolic blood pressures. To explore additional chemicals with chemotaxonomic and therapeutic potentials, the whole root was analyzed via GC and GC-MS, and compounds were isolated and identified. This study first reports the presence of pellitorine, γ-sanshool, asarinin, skimmianine, terpene hydrocarbons, o-hydroxymethyl benzoic acid, and fatty acids in Z. tessmannii root. Identified compounds include amides (pellitorine, fagaramide, γ-sanshool), alkaloids (skimmianine, dihydrochelerythrine, fagaridine), a lignan (asarinin), terpenes (α-pinene, γ-cadinene, etc.), and fatty acids (9,12-octadecadienoate, etc.). Amides are responsible for the root's insecticidal action and pungency; o-hydroxymethyl benzoic acid acts as an antisickling agent, while asarinin and terpene hydrocarbons exhibit antimicrobial activities. The combined GC and GC-MS approach provides a rapid method for screening known constituents of this species.