Axelopran
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Systematic (IUPAC) name | |
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3-[(1R,5S)-8-[2-[cyclohexylmethyl-[(2S)-2,3-dihydroxypropanoyl]amino]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]benzamide
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Identifiers | |
CAS Number | 949904-48-7 949904-50-1 (sulfate) |
ATC code | none |
PubChem | CID 67156338 |
ChemSpider | 31444004 |
Chemical data | |
Formula | C26H39N3O4 |
Molar mass | 457.60556 g/mol |
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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 potent, selective, and peripherally-restricted μ-, κ-, and δ-opioid receptor antagonist, 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.[1]
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