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 949904-50-1 (sulfate) |
ATC code | none |
PubChem | CID 67156338 |
ChemSpider | 31444004 |
Chemical data | |
Formula | C26H39N3O4 |
Molar 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
- ↑ , Axelopran (td-1211) briefing document anesthetic and analgesic drug products advisory committee June 11 and 12, 2014.
|
This article is issued from Wikipedia - version of the Tuesday, April 05, 2016. The text is available under the Creative Commons Attribution/Share Alike but additional terms may apply for the media files.