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Polymethylene tetramines: a new generation of selective muscarinic antagonists

1988; Elsevier BV; Volume: 9; Issue: 6 Linguagem: Inglês

10.1016/0165-6147(88)90089-2

1873-3735

Carlo Melchiorre,

Ion channel regulation and function

There is increasing evidence to support the existence of multiple subtypes of muscarinic receptors. However, the limited selectivity of available ligands has hampered their characterization. Carlo Melchiorre describes structure-activity relationship studies on a series of polymethylene tetramines which have led to the discovery of methoctramine, a potent and highly selective muscarinic antagonist structurally unrelated to all other known muscarinic agonists and antagonists. Methoctramine not only discriminates significantly between M1 and M2 receptors but also has remarkable selectivity for cardiac M2 muscarinic receptors.