• Source: Tripitramine

Tripitramine, or tripitamine, is an antimuscarinic drug which was never marketed.




Pharmacology


The drug is a selective antagonist of the muscarinic acetylcholine M2 receptor. Its affinities (Ki) for the muscarinic acetylcholine receptors are 0.27 nM for the M2 receptor, 1.58 nM for the M1 receptor (5.9-fold less than for M2), 6.41 nM for the M4 receptor (24-fold less than for M2), 33.87 nM for the M5 receptor (125-fold less than for M2), and 38.25 nM for the M3 receptor (142-fold less than for M2). Tripitramine has been found to be cardioselective and to increase heart rate in animals.




Chemistry


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). Related compounds with analogous structural designs include dipitramine, spirotramine, caproctamine, and benextramine, among others.




History


Tripitramine was first described in the scientific literature by 1993. It was developed in efforts to discover more highly selective M2 receptor antagonists than methoctramine.




References

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• Tripitramine
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