Tetrahydropyridine (THP) moiety is a part of many biologically active systems. The discovery of the neurotoxic properties of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) as well as numerous alkaloids, prompted extensive research on the synthesis and pharmacological properties of these compounds. The goal was extending the database for structure-activity relationship (SAR) studies. Consequently, many promising drug candidates were designed and a lot more are under clinical study. The current paper reviews the most popular approaches for the synthesis of THP derivatives. The pharmacological characteristics of some THP derivatives are summarized together with composite of the data from their in vitro, ex vivo and in vivo assays.