Novel molecular targets of dezocine and their clinical implications.

ABSTRACT:

Background

Although dezocine is a partial μ-opioid receptor agonist, it is not a controlled substance. Thus, the characterization of the molecular targets of dezocine is critical for scientific and clinical implications. The goal of this study is to characterize molecular targets for dezocine and determine their implications.

Methods

A binding screen for dezocine was performed on 44 available receptors and transporter proteins. Functional assays for the novel targets were performed along with computation calculations to locate the binding site. A G protein activation study was performed for the human κ opioid receptor to determine whether dezocine is a κ-antagonist. Data are presented as mean ± standard error.

Results

The affinities for dezocine were 3.7 ± 0.7 nM for

SUBMITTER: Liu R 

PROVIDER: S-EPMC3944410 | biostudies-literature | 2014 Mar

REPOSITORIES: biostudies-literature