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 Number	949904-48-7 Template:CAS (sulfate)
ATC code	none
PubChem	CID: 67156338
ChemSpider	31444004
Chemical data
Formula	C26H39N3O4
Molecular mass	457.60556 g/mol
SMILES C1CCC(CC1)CN(CCN2C3CCC2CC(C3)C4=CC=CC(=C4)C(=O)N)C(=O)C(CO)O
InChI InChI=1S/C26H39N3O4/c27-25(32)20-8-4-7-19(13-20)21-14-22-9-10-23(15-21)29(22)12-11-28(26(33)24(31)17-30)16-18-5-2-1-3-6-18/h4,7-8,13,18,21-24,30-31H,1-3,5-6,9-12,14-17H2,(H2,27,32)/t21-,22+,23-,24-/m0/s1 Key:ATLYLVPZNWDJBW-KIHHCIJBSA-N

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.

See also

• Bevenopran
• Eluxadoline
• Methylnaltrexone
• Naldemedine