![A peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95); selective for the μ-opioid receptor over the δ-opioid receptor (Ki = 866 nM); acts as a partial agonist of κ-opioid receptors in vitro (EC50 = 47 nM for [35S]GTPγS binding); reverses morphine-induced decreases in gastrointestinal motility and analgesia in a hot-plate assay in rats (ED50s = 23.1 and 55.4 mg/kg](https://interpriseusa.com/wp-content/uploads/2021/06/23731.png)
Description
A peripherally acting antagonist of the μ-opioid receptor (Ki = 7.42 nM; pA2 = 7.95); selective for the μ-opioid receptor over the δ-opioid receptor (Ki = 866 nM); acts as a partial agonist of κ-opioid receptors in vitro (EC50 = 47 nM for [35S]GTPγS binding); reverses morphine-induced decreases in gastrointestinal motility and analgesia in a hot-plate assay in rats (ED50s = 23.1 and 55.4 mg/kg, respectively); exhibits minimal brain uptake in a rat brain perfusion model
Formal name: (5α,6α)-4,5-epoxy-6-(3,6,9,12,15,18,21-heptaoxadocos-1-yloxy)-17-(2-propen-1-yl)-morphinan-3,14-diol, monoethanedioate
Synonyms: AZ 13337019|NKTR-118
Molecular weight: 741.8
CAS: 1354744-91-4
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Receptor Pharmacology|Agonists||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Neuroscience|Pain Research
