Tabernaemontanine was first reported in 1939[1] but its structure was only fully confirmed in the 1970s as there was confusion in the original literature regarding the configuration of the ethyl group in the piperidine ring of this alkaloid and its isomer dregamine, so that their identities had been reversed.

[2][3][4] Both compounds were isolated from plants of the dogbane (Apocynaceae) family including Tabernaemontana coronaria.

As with other Indole alkaloids, the biosynthesis of tabernaemontanine starts from the amino acid tryptophan.

[12] Plant metabolites have been of interest for their possible biological activity and alkaloids in particular are major subjects for ethnobotanical research.

[13][14] Tabernaemontanine has been studied, for example as a potential anti-cancer agent,[15][16][17][18] for its antimalarial activity[19][20] and in antifertility research.