[1][2][3][4] The drug is a selective antagonist of the muscarinic acetylcholine M2 receptor.

[2][5] Tripitramine has been found to be cardioselective and to increase heart rate in animals.

[1][7] Structurally, it consists of three pirenzepine- or AQ-RA 741-like tricyclic (more specifically pyridobenzodiazepine) moieties bound together by a long amine-containing hydrocarbon chain similar to the one found within methoctramine (a modestly M2-selective antimuscarinic agent).

[1][8][4] Related compounds with analogous structural designs include dipitramine, spirotramine, caproctamine, and benextramine, among others.

[4] It was developed in efforts to discover more highly selective M2 receptor antagonists than methoctramine.