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Axelopran

Axelopran
Systematic (IUPAC) name
3-[(1R,5S)-8-[2-[cyclohexylmethyl-[(2S)-2,3-dihydroxypropanoyl]amino]ethyl]-8-azabicyclo[3.2.1]octan-3-yl]benzamide
Identifiers
CAS Registry Number
949904-50-1 (sulfate)
PubChem CID:
ChemSpider
Chemical data
Formula C26H39N3O4
Molecular mass 457.60556 g/mol

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]

See also

References

  1. ^ [2], AXELOPRAN (TD-1211) BRIEFING DOCUMENT ANESTHETIC AND ANALGESIC DRUG PRODUCTS ADVISORY COMMITTEE JUNE 11 AND 12, 2014.



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