Opioids, receptor agonists and antagonists

Zimmerman DM, Leander JD. Selective opioid receptor agonists and antagonists research tools and potential therapeutic agents. J Med Chem 1990 33 895-902. 

Portoghese P, Moe S, Takemori A. A selective deltal opioid receptor agonist derived from oxymorphone evidence for separate recognition sites for deltal opioid receptor agonists and antagonists. 

Eguchi M. Recent advances in selective opioid receptor agonists and antagonists. Med Res Rev 2004 24 182-212. 

Figure 1 Delta opioid receptor agonists and antagonists.

Portoghese PS, Moe ST, Takemori AE (1993) A selective 51 opioid receptor agonist derivative from oxymorphone. Evidence for separate recognition sites for 51 opioid receptor agonists and antagonists. J Med Chem 36 2572-2574... 

Win 42156-2) is a benzazocin derivative, a mixed OPIOID RECEPTOR AGONIST and OPIOID RECEPTOR ANTAGONIST with OPIOID ANALGESIC activity, tonazocine mesylate tonazocine. 

A 17 amino acid long peptide sequentially related to opioid peptides in particular dynorphin A. OFQ/N is inactive at the 5, k, and p opioid receptors, but binds to its own NOP receptor (formerly ORL-1, for opioid receptor like-1). In contrast to opioid peptides, OFQ/N has no direct analgesic properties. OFQ/N is the first example for the discovery of a novel neurotransmitter from tissue extracts by using an orphan receptor as bait. Centrally administered in rodents, OFQ/N exerts anxiolytic properties. OFQ/N agonists and antagonists... 

Fig. 37.4. Spectral map of the 26 opioid agonists and antagonists in 4 receptor binding tests, as described by Table 37.7 [45, 46]. Circles refer to the compounds. Squares represent the binding tests. Areas of circles and squares are proportional to the marginal mean affinities in the table. The lines that join the three poles (DHM, DADLE and EKC) of the map represent axes of contrast between the p-, 8-and K-opioid receptors. The horizontal and vertical components represent 18 and 79%, respectively, of the interaction in the data.

---