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| Clinical data | |
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| Other names | Tripitamine |
| Drug class | Muscarinic acetylcholine receptor antagonist;Selectivemuscarinic acetylcholineM2 receptorantagonist |
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| CAS Number | |
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| Chemical and physical data | |
| Formula | C64H77N13O6 |
| Molar mass | 1124.405 g·mol−1 |
| 3D model (JSmol) | |
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Tripitramine, ortripitamine, is anantimuscarinicdrug which was never marketed.[1][2][3][4]
The drug is aselectiveantagonist of themuscarinic acetylcholineM2 receptor.[1][2][3][5][6] Itsaffinities (Ki) for the muscarinic acetylcholine receptors are 0.27 nM for the M2 receptor, 1.58 nM for theM1 receptor (5.9-fold less than for M2), 6.41 nM for theM4 receptor (24-fold less than for M2), 33.87 nM for theM5 receptor (125-fold less than for M2), and 38.25 nM for theM3 receptor (142-fold less than for M2).[2][5] Tripitramine has been found to becardioselective and to increaseheart rate in animals.[1][7]
Structurally, it consists of threepirenzepine- orAQ-RA 741-liketricyclic (more specifically pyridobenzodiazepine)moieties bound together by a longamine-containinghydrocarbonchain similar to the one found withinmethoctramine (a modestly M2-selective antimuscarinic agent).[1][8][4] Related compounds with analogous structural designs includedipitramine,spirotramine,caproctamine, andbenextramine, among others.[1]
Tripitramine was first described in thescientific literature by 1993.[4] It was developed in efforts to discover more highly selective M2 receptor antagonists than methoctramine.[1][4]
