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4397 Axelopran
b7a40f98e086d0564381a54fae7517db80f76dc99216b6d6a85a4c65bd902ef3

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Properties

Chemistry

Axelopran (INN, USAN) (developmental code name TD-1211) is a drug which is under development by Theravance Biopharma for the treatment of opioid-induced constipation. It acts as a peripherally acting μ-opioid receptor antagonist and also acts on κ-, and δ-opioid receptors, with similar affinity for the μ- and κ-opioid receptors and about an order of magnitude lower affinity for the δ-opioid receptor. Axelopran has potent μ-opioid receptor antagonist activity on the gastrointestinal tract in vivo, and thus it produces a dose-dependent inhibition of opioid-induced delaying in gastric emptying in mice and rats following subcutaneous or oral administration.

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