Preclinical Assessment of the Analgesic Pharmacology of NKTR-181 in Rodents.

ABSTRACT:

Objective

Pharmacological evaluation of the mu-opioid receptor (MOR) agonist properties of NKTR-181 in rodent models.

Methods

Graded noxious stimulus intensities were used in rats to establish the antinociceptive potency and efficacy of NKTR-181 relative to morphine, fentanyl, and oxycodone. Characteristics of MOR agonist actions, as measured by antinociceptive tolerance and cross-tolerance, as well as opioid-induced hyperalgesia (OIH) and naloxone-precipitated withdrawal in NKTR-181- and morphine-dependent in mice, were compared.

Results

NKTR-181 showed dose- and time-related antinociception with similar maximal effects to morphine in the rat and mouse hot-water tail-flick test. No sex or species differences were observed in NKTR-181 or morphine antinociception. Rats

SUBMITTER: Kopruszinski CM 

PROVIDER: S-EPMC11448559 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature