Chemical Structure : NKTR-181
货号: PC-60802Not For Human Use, Lab Use Only.
A novel, long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold).
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NKTR-181 (Loxicodegol) is a long-acting and orally active, selective mu-opioid agonist that displays higher binding affinity (Ki=237 nM) at the MOR than kappa and delta opioid receptors (>100-fold);.
NKTR-181 demonstrates maximum analgesic activity comparable to that of oxycodone in hot-plate latency and acetic-acid writhing models.
NKTR-181 reduces its rate of entry across the blood-brain barrier compared with traditional mu-opioid agonists.
分子量 | 595.73 | |
分子式 | C31H49NO10 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Miyazaki T, et al. J Pharmacol Exp Ther. 2017 Oct;363(1):104-113.
2. Webster L, et al. Pain Med. 2017 Mar 10. doi: 10.1093/pm/pnw344.
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