Pharmacological Characterization of Levorphanol, a G-Protein Biased Opioid Analgesic.

ABSTRACT:

Background

Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs.

Methods

Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays. In vivo analgesia studies using the radiant heat tail flick assay explored the receptor selectivity of the responses through the use of knockout (KO) mice, selective antagonists, and viral rescue approaches.

Results

Receptor binding studies revealed high levorphanol affinity for all th

SUBMITTER: Le Rouzic V 

PROVIDER: S-EPMC6181797 | biostudies-literature | 2019 Feb

REPOSITORIES: biostudies-literature