Journal: BJA: British Journal of Anaesthesia
Article Title: Development and characterisation of novel fentanyl-delta opioid receptor antagonist based bivalent ligands
doi: 10.1093/bja/aeu454
Figure Lengend Snippet: Agonist and antagonist activity of the [fentanyl]–[Dmt-Tic] bivalent pharmacophores at CHO h MOP and CHO h DOP. Antagonist affinity was determined against Fentanyl (MOP) and DPDPE [D-Pen 2 , D-Pen 5 Enkephalin] (DOP). Relative intrinsic activity was determined by removal of basal activity and as a ratio of full agonist E max . All experiments are represented as the mean ( sem ) with n≥3. If a significant difference was detected ( anova ), post-hoc testing using Bonferroni multiple comparisons was employed * P <0.05; ** P <0.005; **** P <0.0001 compared with fentanyl for MOP and Dmt-Tic for DOP
Article Snippet: Fentanyl, norbinaltorphimine (KOP antagonist, norBNI) and [D-Pen 2 , D-Pen 5 ]-enkephalin (DOP agonist, DPDPE) were purchased from Tocris (Abingdon, UK).
Techniques: Activity Assay