Abstract
The binding selectivity of the muscarinic antagonist tripitramine has been tested on the five cloned human muscarinic receptor subtypes (Hm 1 to Hm 5) expressed in chinese hamster ovary (CHO-K1) cells. The results indicate that tripitramine binds to the muscarinic Hm 2 receptor with a K i value of 0.27 ± 0.02 nM. Tripitramine distinguishes Hm 2 vs. Hm 4 by a factor of 24 and vs. Hm 3 and Hm 5 by a factor of 142 and 125, respectively. A lower affinity ratio, about 6-fold, was found between muscarinic Hm 2 and Hm 1 receptors. A comparative study with the well-known selective muscarinic M 2 receptor antagonist methoctramine indicates that tripitramine has gained both potency and selectivity for the muscarinic Hm 2 receptor subtype.
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